Background: The lack of local availability for drugs in the colon can be addressed by preparing a... more Background: The lack of local availability for drugs in the colon can be addressed by preparing a self-microemulsifying drug delivery system (SMEDDS) of curcumin (Cur) which is ultimately used for the treatment of inflammatory bowel disease (IBD). Methods: From preformulation studies, Lauroglycol FCC (oil), Tween 80 (surfactant), Transcutol HP (co-surfactant), and Avicel (solid carrier) were selected for the preparation of blank liquid and solid Cur-loaded SMEDDSs (S-Cur-SMEDDSs). Results: Z-average size (12.36 ± 0.04 nm), zeta potential (−14.7 ± 0.08 mV), and polydispersity index (PDI) (0.155 ± 0.036) showed a comparative droplet surface area and charge of both SMEDDSs. The physicochemical stability of Cur in S-Cur-SMEDDSs was confirmed via FTIR, DSC, TGA, and XRD analyses, while morphological analysis through SEM and atomic force microscopy (AFM) confirmed Cur loading into SMEDDSs with an increased surface roughness root mean square (RMS) of 11.433 ± 0.91 nm, greater than the blank SMEDDS. Acute toxicity studies with an organ weight ratio and % hemolysis of 15.65 ± 1.32% at a high concentration of 600 mM showed that S-Cur-SMEDDSs are safe at a medium dose (0.2-0.8 g/kg/day). The excellent in vitro antioxidant (68.54 ± 1.42%) and anti-inflammatory properties (56.47 ± 1.17%) of S-Cur-SMEDDS proved its therapeutic efficacy for IBD. Finally, S-Cur-SMEDDS significantly improved acetic acid-induced IBD in albino rats through a reduction in the disease activity index (DAI) and macroscopic ulcer score (MUS) from 4.15 ± 0.21 to 1.62 ± 0.12 at 15 mg/kg/day dose, as confirmed via histopathological assay. Conclusions: Based on the above findings, S-Cur-SMEDDS appears to be a stable, less toxic, and more efficacious alternative for Cur delivery with strong competence in treating IBD.
Pharmaceutical Development and Technology, Jan 7, 2016
To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of... more To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of pediatric anaphylaxis. Four different films have been prepared by solvent casting technique where the percentages of the polymer (Lycoat RS720) were optimized. The polymer percentages were (20%, 25%, 27% and 30%) of the total formulation weighs. The thickness and elastic modulus of the optimized film was evaluated using dynamic mechanical analyzer. Epinephrine content uniformity was assessed using UV at wavelength 280 nm. For the dissolution test, fast dissolving films (FDFs) were evaluated in 500 Simulated Saliva, with 50 rpm. In vivo taste and disintegration evaluation was performed on six healthy volunteers. Films formed by formulations 1, 2 and 3 were too sticky after drying, while formulation 4 that has 30% polymer content formed smooth, transparent, flexible and uniform film, and therefore, it was selected for further testing. The value of elastic modulus was determined at 1.325 MPa. The thickness of the film at different locations was measured at 0.29 mm. Drug content in film was measured at 93% ±10. More than 90% of epinephrine was released from the film within 7.2 min. Bitterness of epinephrine was masked efficiently according to volunteer's comments with average disintegration time of 20 s. This study presents potential proof for using FDFs as a replacement therapy of epinephrine injections for pediatrics.
This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) t... more This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) to improve its solubility and bioavailability via two different techniques; The polymer-based surface solid dispersion (SSD) technique and the solidified surfactant (SS) technique. In the first technique, two polymers were used; polyvinylpyrrolidone (PVP K90) and Poloxamer 407 (Pluronic®F127), while in the second technique the liquid Tween 80 was solidified by adsorption onto Aeroperl®300. The pre-compression and post-compression parameters of the obtained formulations were assessed. The best formulations were subjected to a taste masking evaluation and a short-term stability study. The results demonstrated that, in comparison to the pure drug, the proportion of drug released from each of the prepared FDTs considerably increased. Results of the stability studies showed that the chosen drug formulations remained stable throughout the storage period.
Journal of Drug Delivery Science and Technology, Aug 1, 2020
The present work aims to develop and characterize domperidone resinate complex to be loaded into ... more The present work aims to develop and characterize domperidone resinate complex to be loaded into a gastroretentive delivery system. The formed resinate complex will be used to control the drug release in the stomach from inside the gastroretentive delivery system. Methods: Resinate complexes were formulated by a simple aqueous binding method. Screening of different types of resins was carried out. Domperidone binding study was tested at various drug and resin concentrations. Physicochemical characterizations were carried out to evaluate the prepared resinate complex. These studies included flow properties, in vitro drug release in simulated gastric fluid (SGF), Differential scanning calorimetry (DSC), Mass spectroscopy and XPRD evaluations. Also, the stability study of the selected resinate complex was conducted at 25 � C and 40 � C for up to one month. Results: Domperidone and Dowex 50WX2 in a ratio of 1:3 have formed a resinate complex that has shown acceptable flow properties, thermal properties and short-term chemical stability at 25 � C and 40 � C. Domperidone release profile from resinate in SGF has shown slow controlled release characteristics. Conclusion: The domperidone stable complex with Dowex ion exchange resin has the potential for further development as gastroretentive drug delivery system as a mean of controlling the drug release.
Journal of Drug Delivery Science and Technology, Oct 1, 2020
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Drug Development and Industrial Pharmacy, Mar 17, 2016
Abstract Purpose: To evaluate the physicochemical characteristics of clindamycin HCl in a complex... more Abstract Purpose: To evaluate the physicochemical characteristics of clindamycin HCl in a complex form (resinate) with ion exchange resin (IER) (Amberlite IRP69). Methods: Drug–resin complex was prepared by simple aqueous binding method. Drug binding study was carried out at different drug and resin concentrations. Several physicochemical characterization studies were conducted to evaluate the resinate complex. These studies included flow properties, in vitro drug release in SGF and SIF, DSC, TGA, mass spectroscopy and XPRD evaluations. In addition, stability study of resinate complex was conducted at 25 and 40 °C for up to 1 month. Results: Clindamycin and Amberlite IRP69 have formed a complex (resinate) and have shown good flow properties, good thermal properties and chemical stability (short term over 4 weeks) at 25 and 40 °C. Clindamycin release profiles from resinate in SGF and SIF have shown immediate release characteristics and release in simulated saliva has shown dependence on water volume. Conclusion: The clindamycin stable complex with IER (Amberlite IRP69) has the potential for further development as a compatible pediatric liquid formulation (suspension) or a fast disintegrating tablet.
Drug Development and Industrial Pharmacy, Mar 28, 2016
To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. S... more To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. Several types of Ion exchange resins were screened for their binding efficiency with clindamycin. In order to develop a suspension formulation, several thickening agents, surfactants, sweeting and flavoring agents, were evaluated for their influence on the release of clindamycin from resinate. Rheological studies were also conducted to select the optimum amounts of the suspending agents. The release profiles of clindamycin in SGF and SIF were also evaluated from freshly prepared suspension and from suspension formulation after storage for one month at 25°C and 40°C. Clindamycin bitterness threshold was determined based on volunteers' evaluation, and taste evaluation was conducted in 12 adult volunteers who evaluated the taste of the optimized suspension against clindamycin solution. Among all resins tested, Amberlite IRP 69 showed the highest binding efficiency to clindamycin. Several excipients were selected into the suspension formulation based on no or minimum influence on the release of clindamycin from the resinate complex. Moreover, xanthan gum was selected as the optimal suspending agent for the suspension. Clindamycin release profiles in SGF or SIF showed 90% release within 30 minutes from freshly prepared sample. Clindamycin exhibited good stability profiles at 25°C and 40°Cover one month storage. The mean bitterness threshold of clindamycin was 12.5μg/ml, and taste evaluation study in adults showed sustainable taste improvement for suspension over clindamycin solution. Clindamycin/Resin complexation has shown to be an efficient method to mask the taste of clindamycin and was developed into a suspension formulation that can be used in pediatrics.
The global state of antibiotic resistance highlights the necessity for new drugs that can treat a... more The global state of antibiotic resistance highlights the necessity for new drugs that can treat a wide range of microbial infections.
The global state of antibiotic resistance highlights the necessity for new drugs that can treat a... more The global state of antibiotic resistance highlights the necessity for new drugs that can treat a wide range of microbial infections. Drug repurposing has several advantages, including lower costs and improved safety compared to developing a new compound. The aim of the current study is to evaluate the repurposed antimicrobial activity of Brimonidine tartrate (BT), a well-known antiglaucoma drug, and to potentiate its antimicrobial effect by using electrospun nanofibrous scaffolds. BT-loaded nanofibers were fabricated in different drug concentrations (1.5, 3, 6, and 9%) via the electrospinning technique using two biopolymers (PCL and PVP). Then, the prepared nanofibers were characterized by SEM, XRD, FTIR, swelling ratio, and in vitro drug release. Afterward, the antimicrobial activities of the prepared nanofibers were investigated in vitro using different methods against several human pathogens and compared to the free BT. The results showed that all nanofibers were prepared successfully with a smooth surface. The diameters of nanofibers were reduced after loading of BT compared to the unloaded ones. In addition, scaffolds showed controlled-drug release profiles that were maintained for more than 7 days. The in vitro antimicrobial assessments revealed good activities for all scaffolds against most of the investigated human pathogens, particularly the one prepared with 9% BT which showed superiority in the antimicrobial effect over other scaffolds. To conclude, our findings proved the capability of nanofibers in loading BT and improving its repurposed antimicrobial efficacy. Therefore, it could be a promising carrier for BT to be used in combating numerous human pathogens.
This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) t... more This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) to improve its solubility and bioavailability via two different techniques; the polymer-based surface solid dispersion (SSD) technique and the solidified surfactant (SS) technique. In the first technique, two polymers were used; polyvinylpyrrolidone (PVP K90) and Poloxamer 407 (Pluronic®F127), while in the second technique the liquid Tween 80 was solidified by adsorption onto Aeroperl®300. The pre-compression and post-compression parameters of the obtained formulations were assessed. The best formulations were subjected to a taste masking evaluation and a shortterm stability study. The results demonstrated that, in comparison to the pure drug, the proportion of drug released from each of the prepared FDTs considerably increased. Results of the stability studies showed that the chosen drug formulations remained stable throughout the storage period.
Journal of Drug Delivery Science and Technology, 2020
Abstract This work aims to develop and evaluate buoyant beads embedded with domperidone/Dowex 50W... more Abstract This work aims to develop and evaluate buoyant beads embedded with domperidone/Dowex 50WX2 resinate complex as novel multiple-unit type oral gastro-retentive drug delivery system. Domperidone (BCS II) has been chosen for gastric retention as it has a poor oral bioavailability (around 15%), a short biological half-life, and pH-dependent solubility with poor solubility at a high pH and good solubility at low pH. Two different techniques were used to induce beads buoyancy; first, formulation of effervescent beads by incorporation of NaHCO3 in the beads, which will release carbon dioxide gas upon reaction with the acidic gastric fluid causing the beads to float. Second, is the formation of low-density emulgel beads by the incorporation of light mineral oil in the beads. Resinate complex is used to control the drug release from the prepared formulations. Beads were evaluated for percent drug entrapment efficiency, floating behavior (float lag time and duration), mean particle diameter, in vitro drug release, and release kinetics in SGF. The effect of different concentrations of both NaHCO3 (1%, 2%, and 10%) and light mineral oil (2%, 5%, and 10%) on the floating behavior and physical appearance was studied. The optimized formula (F10) was subjected to a four-week stability study at both 25 oC and 40 oC. Results revealed that gastro-retentive beads possessed a floating duration of up to 24 hours and no floating lag time was developed. The novel resinate loaded beads succeeded to sustain the release of domperidone in SGF. The optimized formula was stable at both temperatures of 25 oC and 40 oC for four weeks. Hence, the developed optimized formulation (F10) is considered as a potential to increase the domperidone bioavailability, decrease dosage frequency, and increase patient compliance.
Journal of Drug Delivery Science and Technology, 2020
Abstract Purpose The present work aims to develop and characterize domperidone resinate complex t... more Abstract Purpose The present work aims to develop and characterize domperidone resinate complex to be loaded into a gastroretentive delivery system. The formed resinate complex will be used to control the drug release in the stomach from inside the gastroretentive delivery system. Methods Resinate complexes were formulated by a simple aqueous binding method. Screening of different types of resins was carried out. Domperidone binding study was tested at various drug and resin concentrations. Physicochemical characterizations were carried out to evaluate the prepared resinate complex. These studies included flow properties, in vitro drug release in simulated gastric fluid (SGF), Differential scanning calorimetry (DSC), Mass spectroscopy and XPRD evaluations. Also, the stability study of the selected resinate complex was conducted at 25 °C and 40 °C for up to one month. Results Domperidone and Dowex 50WX2 in a ratio of 1:3 have formed a resinate complex that has shown acceptable flow properties, thermal properties and short-term chemical stability at 25 °C and 40 °C. Domperidone release profile from resinate in SGF has shown slow controlled release characteristics. Conclusion The domperidone stable complex with Dowex ion exchange resin has the potential for further development as gastroretentive drug delivery system as a mean of controlling the drug release.
To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. S... more To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. Several types of Ion exchange resins were screened for their binding efficiency with clindamycin. In order to develop a suspension formulation, several thickening agents, surfactants, sweeting and flavoring agents, were evaluated for their influence on the release of clindamycin from resinate. Rheological studies were also conducted to select the optimum amounts of the suspending agents. The release profiles of clindamycin in SGF and SIF were also evaluated from freshly prepared suspension and from suspension formulation after storage for one month at 25°C and 40°C. Clindamycin bitterness threshold was determined based on volunteers' evaluation, and taste evaluation was conducted in 12 adult volunteers who evaluated the taste of the optimized suspension against clindamycin solution. Among all resins tested, Amberlite IRP 69 showed the highest binding efficiency to clindamycin. Several...
Pharmaceutical development and technology, Jan 7, 2016
To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of... more To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of pediatric anaphylaxis. Four different films have been prepared by solvent casting technique where the percentages of the polymer (Lycoat RS720) were optimized. The polymer percentages were (20%, 25%, 27% and 30%) of the total formulation weighs. The thickness and elastic modulus of the optimized film was evaluated using dynamic mechanical analyzer. Epinephrine content uniformity was assessed using UV at wavelength 280 nm. For the dissolution test, fast dissolving films (FDFs) were evaluated in 500 Simulated Saliva, with 50 rpm. In vivo taste and disintegration evaluation was performed on six healthy volunteers. Films formed by formulations 1, 2 and 3 were too sticky after drying, while formulation 4 that has 30% polymer content formed smooth, transparent, flexible and uniform film, and therefore, it was selected for further testing. The value of elastic modulus was determined at 1.325 M...
Drug Development and Industrial Pharmacy, Mar 17, 2016
To evaluate the physicochemical characteristics of clindamycin HCl in a complex form (resinate) w... more To evaluate the physicochemical characteristics of clindamycin HCl in a complex form (resinate) with ion exchange resin (Amberlite IRP69). Drug-resin complex was prepared by simple aqueous binding method. Drug binding study was carried out at different drug and resin concentrations. Several physicochemical characterization studies were conducted to evaluate the resinate complex. These studies included flow properties, in vitro drug release in SGF and SIF, DSC, TGA, Mass spectroscopy and XPRD evaluations. In addition, stability study of resinate complex was conducted at 25(o)C and 40(o)C for up to one month. Clindamycin and Amberlite IRP69 have formed a complex (resinate) and has shown good flow properties, good thermal properties and chemical stability (short term over 4 weeks) at 25(o)C and 40(o)C. Clindamycin release profiles from resinate in SGF and SIF has shown immediate release characteristics and release in simulated saliva has shown dependence on water volume. The clindamycin stable complex with ion exchange resin (Amberlite IRP69) has the potential for further development as a compatible pediatric liquid formulation (suspension) or a fast disintegrating tablet.
Background: The lack of local availability for drugs in the colon can be addressed by preparing a... more Background: The lack of local availability for drugs in the colon can be addressed by preparing a self-microemulsifying drug delivery system (SMEDDS) of curcumin (Cur) which is ultimately used for the treatment of inflammatory bowel disease (IBD). Methods: From preformulation studies, Lauroglycol FCC (oil), Tween 80 (surfactant), Transcutol HP (co-surfactant), and Avicel (solid carrier) were selected for the preparation of blank liquid and solid Cur-loaded SMEDDSs (S-Cur-SMEDDSs). Results: Z-average size (12.36 ± 0.04 nm), zeta potential (−14.7 ± 0.08 mV), and polydispersity index (PDI) (0.155 ± 0.036) showed a comparative droplet surface area and charge of both SMEDDSs. The physicochemical stability of Cur in S-Cur-SMEDDSs was confirmed via FTIR, DSC, TGA, and XRD analyses, while morphological analysis through SEM and atomic force microscopy (AFM) confirmed Cur loading into SMEDDSs with an increased surface roughness root mean square (RMS) of 11.433 ± 0.91 nm, greater than the blank SMEDDS. Acute toxicity studies with an organ weight ratio and % hemolysis of 15.65 ± 1.32% at a high concentration of 600 mM showed that S-Cur-SMEDDSs are safe at a medium dose (0.2-0.8 g/kg/day). The excellent in vitro antioxidant (68.54 ± 1.42%) and anti-inflammatory properties (56.47 ± 1.17%) of S-Cur-SMEDDS proved its therapeutic efficacy for IBD. Finally, S-Cur-SMEDDS significantly improved acetic acid-induced IBD in albino rats through a reduction in the disease activity index (DAI) and macroscopic ulcer score (MUS) from 4.15 ± 0.21 to 1.62 ± 0.12 at 15 mg/kg/day dose, as confirmed via histopathological assay. Conclusions: Based on the above findings, S-Cur-SMEDDS appears to be a stable, less toxic, and more efficacious alternative for Cur delivery with strong competence in treating IBD.
Pharmaceutical Development and Technology, Jan 7, 2016
To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of... more To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of pediatric anaphylaxis. Four different films have been prepared by solvent casting technique where the percentages of the polymer (Lycoat RS720) were optimized. The polymer percentages were (20%, 25%, 27% and 30%) of the total formulation weighs. The thickness and elastic modulus of the optimized film was evaluated using dynamic mechanical analyzer. Epinephrine content uniformity was assessed using UV at wavelength 280 nm. For the dissolution test, fast dissolving films (FDFs) were evaluated in 500 Simulated Saliva, with 50 rpm. In vivo taste and disintegration evaluation was performed on six healthy volunteers. Films formed by formulations 1, 2 and 3 were too sticky after drying, while formulation 4 that has 30% polymer content formed smooth, transparent, flexible and uniform film, and therefore, it was selected for further testing. The value of elastic modulus was determined at 1.325 MPa. The thickness of the film at different locations was measured at 0.29 mm. Drug content in film was measured at 93% ±10. More than 90% of epinephrine was released from the film within 7.2 min. Bitterness of epinephrine was masked efficiently according to volunteer's comments with average disintegration time of 20 s. This study presents potential proof for using FDFs as a replacement therapy of epinephrine injections for pediatrics.
This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) t... more This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) to improve its solubility and bioavailability via two different techniques; The polymer-based surface solid dispersion (SSD) technique and the solidified surfactant (SS) technique. In the first technique, two polymers were used; polyvinylpyrrolidone (PVP K90) and Poloxamer 407 (Pluronic®F127), while in the second technique the liquid Tween 80 was solidified by adsorption onto Aeroperl®300. The pre-compression and post-compression parameters of the obtained formulations were assessed. The best formulations were subjected to a taste masking evaluation and a short-term stability study. The results demonstrated that, in comparison to the pure drug, the proportion of drug released from each of the prepared FDTs considerably increased. Results of the stability studies showed that the chosen drug formulations remained stable throughout the storage period.
Journal of Drug Delivery Science and Technology, Aug 1, 2020
The present work aims to develop and characterize domperidone resinate complex to be loaded into ... more The present work aims to develop and characterize domperidone resinate complex to be loaded into a gastroretentive delivery system. The formed resinate complex will be used to control the drug release in the stomach from inside the gastroretentive delivery system. Methods: Resinate complexes were formulated by a simple aqueous binding method. Screening of different types of resins was carried out. Domperidone binding study was tested at various drug and resin concentrations. Physicochemical characterizations were carried out to evaluate the prepared resinate complex. These studies included flow properties, in vitro drug release in simulated gastric fluid (SGF), Differential scanning calorimetry (DSC), Mass spectroscopy and XPRD evaluations. Also, the stability study of the selected resinate complex was conducted at 25 � C and 40 � C for up to one month. Results: Domperidone and Dowex 50WX2 in a ratio of 1:3 have formed a resinate complex that has shown acceptable flow properties, thermal properties and short-term chemical stability at 25 � C and 40 � C. Domperidone release profile from resinate in SGF has shown slow controlled release characteristics. Conclusion: The domperidone stable complex with Dowex ion exchange resin has the potential for further development as gastroretentive drug delivery system as a mean of controlling the drug release.
Journal of Drug Delivery Science and Technology, Oct 1, 2020
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Drug Development and Industrial Pharmacy, Mar 17, 2016
Abstract Purpose: To evaluate the physicochemical characteristics of clindamycin HCl in a complex... more Abstract Purpose: To evaluate the physicochemical characteristics of clindamycin HCl in a complex form (resinate) with ion exchange resin (IER) (Amberlite IRP69). Methods: Drug–resin complex was prepared by simple aqueous binding method. Drug binding study was carried out at different drug and resin concentrations. Several physicochemical characterization studies were conducted to evaluate the resinate complex. These studies included flow properties, in vitro drug release in SGF and SIF, DSC, TGA, mass spectroscopy and XPRD evaluations. In addition, stability study of resinate complex was conducted at 25 and 40 °C for up to 1 month. Results: Clindamycin and Amberlite IRP69 have formed a complex (resinate) and have shown good flow properties, good thermal properties and chemical stability (short term over 4 weeks) at 25 and 40 °C. Clindamycin release profiles from resinate in SGF and SIF have shown immediate release characteristics and release in simulated saliva has shown dependence on water volume. Conclusion: The clindamycin stable complex with IER (Amberlite IRP69) has the potential for further development as a compatible pediatric liquid formulation (suspension) or a fast disintegrating tablet.
Drug Development and Industrial Pharmacy, Mar 28, 2016
To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. S... more To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. Several types of Ion exchange resins were screened for their binding efficiency with clindamycin. In order to develop a suspension formulation, several thickening agents, surfactants, sweeting and flavoring agents, were evaluated for their influence on the release of clindamycin from resinate. Rheological studies were also conducted to select the optimum amounts of the suspending agents. The release profiles of clindamycin in SGF and SIF were also evaluated from freshly prepared suspension and from suspension formulation after storage for one month at 25°C and 40°C. Clindamycin bitterness threshold was determined based on volunteers' evaluation, and taste evaluation was conducted in 12 adult volunteers who evaluated the taste of the optimized suspension against clindamycin solution. Among all resins tested, Amberlite IRP 69 showed the highest binding efficiency to clindamycin. Several excipients were selected into the suspension formulation based on no or minimum influence on the release of clindamycin from the resinate complex. Moreover, xanthan gum was selected as the optimal suspending agent for the suspension. Clindamycin release profiles in SGF or SIF showed 90% release within 30 minutes from freshly prepared sample. Clindamycin exhibited good stability profiles at 25°C and 40°Cover one month storage. The mean bitterness threshold of clindamycin was 12.5μg/ml, and taste evaluation study in adults showed sustainable taste improvement for suspension over clindamycin solution. Clindamycin/Resin complexation has shown to be an efficient method to mask the taste of clindamycin and was developed into a suspension formulation that can be used in pediatrics.
The global state of antibiotic resistance highlights the necessity for new drugs that can treat a... more The global state of antibiotic resistance highlights the necessity for new drugs that can treat a wide range of microbial infections.
The global state of antibiotic resistance highlights the necessity for new drugs that can treat a... more The global state of antibiotic resistance highlights the necessity for new drugs that can treat a wide range of microbial infections. Drug repurposing has several advantages, including lower costs and improved safety compared to developing a new compound. The aim of the current study is to evaluate the repurposed antimicrobial activity of Brimonidine tartrate (BT), a well-known antiglaucoma drug, and to potentiate its antimicrobial effect by using electrospun nanofibrous scaffolds. BT-loaded nanofibers were fabricated in different drug concentrations (1.5, 3, 6, and 9%) via the electrospinning technique using two biopolymers (PCL and PVP). Then, the prepared nanofibers were characterized by SEM, XRD, FTIR, swelling ratio, and in vitro drug release. Afterward, the antimicrobial activities of the prepared nanofibers were investigated in vitro using different methods against several human pathogens and compared to the free BT. The results showed that all nanofibers were prepared successfully with a smooth surface. The diameters of nanofibers were reduced after loading of BT compared to the unloaded ones. In addition, scaffolds showed controlled-drug release profiles that were maintained for more than 7 days. The in vitro antimicrobial assessments revealed good activities for all scaffolds against most of the investigated human pathogens, particularly the one prepared with 9% BT which showed superiority in the antimicrobial effect over other scaffolds. To conclude, our findings proved the capability of nanofibers in loading BT and improving its repurposed antimicrobial efficacy. Therefore, it could be a promising carrier for BT to be used in combating numerous human pathogens.
This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) t... more This study aims to formulate Olmesartan medoxomil (OM) into oral fast-dissolving tablets (FDTs) to improve its solubility and bioavailability via two different techniques; the polymer-based surface solid dispersion (SSD) technique and the solidified surfactant (SS) technique. In the first technique, two polymers were used; polyvinylpyrrolidone (PVP K90) and Poloxamer 407 (Pluronic®F127), while in the second technique the liquid Tween 80 was solidified by adsorption onto Aeroperl®300. The pre-compression and post-compression parameters of the obtained formulations were assessed. The best formulations were subjected to a taste masking evaluation and a shortterm stability study. The results demonstrated that, in comparison to the pure drug, the proportion of drug released from each of the prepared FDTs considerably increased. Results of the stability studies showed that the chosen drug formulations remained stable throughout the storage period.
Journal of Drug Delivery Science and Technology, 2020
Abstract This work aims to develop and evaluate buoyant beads embedded with domperidone/Dowex 50W... more Abstract This work aims to develop and evaluate buoyant beads embedded with domperidone/Dowex 50WX2 resinate complex as novel multiple-unit type oral gastro-retentive drug delivery system. Domperidone (BCS II) has been chosen for gastric retention as it has a poor oral bioavailability (around 15%), a short biological half-life, and pH-dependent solubility with poor solubility at a high pH and good solubility at low pH. Two different techniques were used to induce beads buoyancy; first, formulation of effervescent beads by incorporation of NaHCO3 in the beads, which will release carbon dioxide gas upon reaction with the acidic gastric fluid causing the beads to float. Second, is the formation of low-density emulgel beads by the incorporation of light mineral oil in the beads. Resinate complex is used to control the drug release from the prepared formulations. Beads were evaluated for percent drug entrapment efficiency, floating behavior (float lag time and duration), mean particle diameter, in vitro drug release, and release kinetics in SGF. The effect of different concentrations of both NaHCO3 (1%, 2%, and 10%) and light mineral oil (2%, 5%, and 10%) on the floating behavior and physical appearance was studied. The optimized formula (F10) was subjected to a four-week stability study at both 25 oC and 40 oC. Results revealed that gastro-retentive beads possessed a floating duration of up to 24 hours and no floating lag time was developed. The novel resinate loaded beads succeeded to sustain the release of domperidone in SGF. The optimized formula was stable at both temperatures of 25 oC and 40 oC for four weeks. Hence, the developed optimized formulation (F10) is considered as a potential to increase the domperidone bioavailability, decrease dosage frequency, and increase patient compliance.
Journal of Drug Delivery Science and Technology, 2020
Abstract Purpose The present work aims to develop and characterize domperidone resinate complex t... more Abstract Purpose The present work aims to develop and characterize domperidone resinate complex to be loaded into a gastroretentive delivery system. The formed resinate complex will be used to control the drug release in the stomach from inside the gastroretentive delivery system. Methods Resinate complexes were formulated by a simple aqueous binding method. Screening of different types of resins was carried out. Domperidone binding study was tested at various drug and resin concentrations. Physicochemical characterizations were carried out to evaluate the prepared resinate complex. These studies included flow properties, in vitro drug release in simulated gastric fluid (SGF), Differential scanning calorimetry (DSC), Mass spectroscopy and XPRD evaluations. Also, the stability study of the selected resinate complex was conducted at 25 °C and 40 °C for up to one month. Results Domperidone and Dowex 50WX2 in a ratio of 1:3 have formed a resinate complex that has shown acceptable flow properties, thermal properties and short-term chemical stability at 25 °C and 40 °C. Domperidone release profile from resinate in SGF has shown slow controlled release characteristics. Conclusion The domperidone stable complex with Dowex ion exchange resin has the potential for further development as gastroretentive drug delivery system as a mean of controlling the drug release.
To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. S... more To develop an oral suspension of clindamycin resin complex for the potential use in pediatrics. Several types of Ion exchange resins were screened for their binding efficiency with clindamycin. In order to develop a suspension formulation, several thickening agents, surfactants, sweeting and flavoring agents, were evaluated for their influence on the release of clindamycin from resinate. Rheological studies were also conducted to select the optimum amounts of the suspending agents. The release profiles of clindamycin in SGF and SIF were also evaluated from freshly prepared suspension and from suspension formulation after storage for one month at 25°C and 40°C. Clindamycin bitterness threshold was determined based on volunteers' evaluation, and taste evaluation was conducted in 12 adult volunteers who evaluated the taste of the optimized suspension against clindamycin solution. Among all resins tested, Amberlite IRP 69 showed the highest binding efficiency to clindamycin. Several...
Pharmaceutical development and technology, Jan 7, 2016
To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of... more To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of pediatric anaphylaxis. Four different films have been prepared by solvent casting technique where the percentages of the polymer (Lycoat RS720) were optimized. The polymer percentages were (20%, 25%, 27% and 30%) of the total formulation weighs. The thickness and elastic modulus of the optimized film was evaluated using dynamic mechanical analyzer. Epinephrine content uniformity was assessed using UV at wavelength 280 nm. For the dissolution test, fast dissolving films (FDFs) were evaluated in 500 Simulated Saliva, with 50 rpm. In vivo taste and disintegration evaluation was performed on six healthy volunteers. Films formed by formulations 1, 2 and 3 were too sticky after drying, while formulation 4 that has 30% polymer content formed smooth, transparent, flexible and uniform film, and therefore, it was selected for further testing. The value of elastic modulus was determined at 1.325 M...
Drug Development and Industrial Pharmacy, Mar 17, 2016
To evaluate the physicochemical characteristics of clindamycin HCl in a complex form (resinate) w... more To evaluate the physicochemical characteristics of clindamycin HCl in a complex form (resinate) with ion exchange resin (Amberlite IRP69). Drug-resin complex was prepared by simple aqueous binding method. Drug binding study was carried out at different drug and resin concentrations. Several physicochemical characterization studies were conducted to evaluate the resinate complex. These studies included flow properties, in vitro drug release in SGF and SIF, DSC, TGA, Mass spectroscopy and XPRD evaluations. In addition, stability study of resinate complex was conducted at 25(o)C and 40(o)C for up to one month. Clindamycin and Amberlite IRP69 have formed a complex (resinate) and has shown good flow properties, good thermal properties and chemical stability (short term over 4 weeks) at 25(o)C and 40(o)C. Clindamycin release profiles from resinate in SGF and SIF has shown immediate release characteristics and release in simulated saliva has shown dependence on water volume. The clindamycin stable complex with ion exchange resin (Amberlite IRP69) has the potential for further development as a compatible pediatric liquid formulation (suspension) or a fast disintegrating tablet.
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