International Journal of Pharmacy and Pharmaceutical Sciences, Jan 1, 2017
Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance ... more Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs. Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients. Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.
International journal of pharma and bio sciences, 2015
Challenges confronting the locally manufactured medications in Saudi Arabia have been increasing ... more Challenges confronting the locally manufactured medications in Saudi Arabia have been increasing in the last decade. The Saudi market is mainly built on imported medications. Meanwhile, local manufacturers are much neglected in the Saudi's market. Building consumer's trust for local medication is one of the main targets to achieve success in decreasing the rate of importing medication while increasing locally produced ones. This study aims to compare the quality of some of the marketed low dose enteric coated Aspirin tablets (as a model product) produced by local Saudi pharmaceutical companies (F1 and F3) with others manufactured by an Arabian Emirate company (F5), and two other brands of USA companies (F2 and F4) as global generics. F2 represents the proprietary product produced by Bayer (Bayer Aspirin ® ), to which all other brands were compared. Different quality control tests adopted by the United States Pharmacopeia and/or the British Pharmacopeia were applied to the fi...
Bioadhesive ophthalmic inserts were prepared using single polymer, namely: hydroxypropylmethyl ce... more Bioadhesive ophthalmic inserts were prepared using single polymer, namely: hydroxypropylmethyl cellulose (HPMC), sodium carboxymethyl cellulose (NaCMC), and sodium alginate (SA) in 2% concentration or a mixture of two polymers. The prepared inserts were evaluated in vitro for content uniformity, thickness, folding endurance, weight variation, surface pH, swelling behavior, bioadhesion, in vitro residence time, and drug release. Inserts were evaluated in vivo for intraocular pressure (IOP) lowering effect, in vivo ocular irritancy, and precorneal residence time. In vitro release study exhibited extended release for 8 h. Inserts based on NaCMC were superior over other inserts with respect to swelling, bioadhesion and extended release. Adding HPMC or NaCMC to SA and adding NaCMC to HPMC improved the characteristics of SA and HPMC inserts, respectively. All inserts showed a significant IOP lowering in normotensive rabbits. SA based inserts showed a stable IOP lowering effect for 5 h.
There has been an increasing demand for the development of nanocarriers targeting multiple diseas... more There has been an increasing demand for the development of nanocarriers targeting multiple diseases with a broad range of properties. Due to their tiny size, giant surface area and feasible targetability, nanocarriers have optimized efficacy, decreased side effects and improved stability over conventional drug dosage forms. There are diverse types of nanocarriers that have been synthesized for drug delivery, including dendrimers, liposomes, solid lipid nanoparticles, polymersomes, polymer–drug conjugates, polymeric nanoparticles, peptide nanoparticles, micelles, nanoemulsions, nanospheres, nanocapsules, nanoshells, carbon nanotubes and gold nanoparticles, etc. Several characterization techniques have been proposed and used over the past few decades to control and predict the behavior of nanocarriers both in vitro and in vivo. In this review, we describe some fundamental in vitro, ex vivo, in situ and in vivo characterization methods for most nanocarriers, emphasizing their advantage...
INTRODUCTION: Free palatal and sub-epithelial connective tissue grafts are the most commonly used... more INTRODUCTION: Free palatal and sub-epithelial connective tissue grafts are the most commonly used grafts in periodontal plastic surgeries. The surgical technique of free palatal grafting requires harvesting of soft tissue from the palatal donor site and transplantation to an intraoral recipient one. Post-surgical complications and atypical healing processes have been described in the literature. In order to reduce the morbidity associated with mucogingival surgery, there are several ways to manage the donor site after soft tissue harvesting. Various topically applied formulas and hemostatic agents have been employed to manage post-operative healing at the donor site. OBJECTIVES: to assess the effects of Calendula based topical formula on palatal wound healing after free palatal graft surgery in comparison to oxidized regenerated cellulose. MATERIAL AND METHODS This randomized, controlled trial included twenty-four surgical sites for palatal graft procurement, divided equally into tw...
Natural pharmaceutical excipients have been applied extensively in the past decades owing to thei... more Natural pharmaceutical excipients have been applied extensively in the past decades owing to their safety and biocompatibility. Zein, a natural protein of plant origin offers great benefit over other synthetic polymers used in controlled drug and biomedical delivery systems. It was used in a variety of medical fields including pharmaceutical and biomedical drug targeting, vaccine, tissue engineering, and gene delivery. Being biodegradable and biocompatible, the current review focuses on the history and the medical application of zein as an attractive still promising biopolymer. Areas covered: The current review gives a broadscope on zein as a still promising protein excipient in different fields. Zein- based drug and biomedical delivery systems are discussed with special focus on current and potential application in controlled drug delivery systems, and tissue engineering. Expert opinion: Zein as a protein of natural origin can still be considered a promising polymer in the field of...
International Journal of Pharmacy and Pharmaceutical Sciences
Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance ... more Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs. Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients. Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.
International Journal of Pharmacy and Pharmaceutical Sciences
Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance ... more Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs. Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients. Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.
Oral candidiasis may be manifested in the oral cavity as either mild or severe oral fungal infect... more Oral candidiasis may be manifested in the oral cavity as either mild or severe oral fungal infection. This infection results from the overgrowth of Candida species normally existing in the oral cavity in minute amounts based on many predisposing factors. Several aspects have spurred the search for new strategies in the treatment of oral candidiasis, among which are the limited numbers of new antifungal drugs developed in recent years. Previous studies have shown that thyme and clove oils have antimycotic activities and have suggested their incorporation into pharmaceutical preparations. This study aimed to investigate the possibility of the incorporation and characterization of essential oils or their extracted active ingredients in Orabase formulations. Orabase loaded with clove oil, thyme oil, eugenol, and thymol were prepared and evaluated for their antifungal activities, pH, viscosity, erosion and water uptake characteristics, mechanical properties, in vitro release behavior, and ex vivo mucoadhesion properties. All prepared bases showed considerable antifungal activity and acceptable physical characteristics. The release pattern from loaded bases was considerably slow for all oils and active ingredients. All bases showed appreciable adhesion in the in vitro and ex vivo studies. The incorporation of essential oils in Orabase could help in future drug delivery design, with promising outcomes on patients' well-being.
Periodontitis is one of the most important chronic inflammatory dental diseases arising from the ... more Periodontitis is one of the most important chronic inflammatory dental diseases arising from the destructive actions caused by a variety of pathogenic organisms presented in the oral cavity. The aim of this study is the preparation and in vitro evaluation of films for the local treatment of periodontal pockets. The prepared films contained either metronidazole (Mtr), for its antimicrobial effect in periodontal diseases, using a mixture of polymers namely hydroxypropyl methyl cellulose, Carbopol 934 or locally applied Pentoxifylline (PTX), for its anti-inflammatory activity, using chitosan. All films were prepared using solvent casting technique and were evaluated for their physical characteristics, drug content uniformity, surface pH, swelling behavior, mechanical properties and in vitro release. Further characterization was done on the selected formulations using differential scanning calorimetry and scanning electron microscopy for surface structure. Clinical evaluation tests were also performed. Appropriate physical characteristics and mechanical properties for most formulations and their suitability for periodontal application were observed. In vitro drug release from most films showed a burst release rate for both Mtr and PTX during the first 2 h after which the release rate was markedly decreased. Clinical trials on patients revealed the advantageous use of Mtr and PTX as an adjunct treatment with traditionally used dental techniques. The effectiveness of the co-therapy of either drug could add benefit in the eradication of chronic periodontal hazards.
Abstract The aim of this study was to formulate Pentoxyfylline drug (PTX) as a local bioadhesive ... more Abstract The aim of this study was to formulate Pentoxyfylline drug (PTX) as a local bioadhesive Carbopol (Cbp) based gels for the aid of bone induction around an endosseus oral implant. The local delivery of the drug will probably avoid most of the problems associated with its systemic use including; disturbances in gastrointestinal tract and the central nervous system. Two concentrations of 1% and 3% Cbp containing 1% PTX were prepared. The gels were investigated for their physicochemical properties. Cbp based gels were found to be translucent with good homogeneity, uniform distribution of the drug and absence of any lumps. The pH of the gels was within neutrality, 7.1, which is considered to be acceptable to avoid the risk of any possible irritation in the oral cavity. The Cbp gels exhibited satisfactory bioadhesive properties and a pseudo-plastic rheological behavior. Cumulative drug released from the gels showed a controlled-release for more than 24 hours with the order of 3% >1% and the drug was released by diffusion mechanism from both gels. Statistical analysis revealed non-significant difference in drug content, rheological property and release rate of the stored gels for six months compared to the fresh ones. In vivo experimental results in rabbits have shown significant difference in bone depth induction of 3% and 1% Cbp gels with the formation of strong organized bone over the control group. Local administration of Pentoxifylline could be regarded as a valid approach in the management of osseointegration.
International Journal of Pharmacy and Pharmaceutical Sciences, Jan 1, 2017
Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance ... more Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs. Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients. Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.
International journal of pharma and bio sciences, 2015
Challenges confronting the locally manufactured medications in Saudi Arabia have been increasing ... more Challenges confronting the locally manufactured medications in Saudi Arabia have been increasing in the last decade. The Saudi market is mainly built on imported medications. Meanwhile, local manufacturers are much neglected in the Saudi's market. Building consumer's trust for local medication is one of the main targets to achieve success in decreasing the rate of importing medication while increasing locally produced ones. This study aims to compare the quality of some of the marketed low dose enteric coated Aspirin tablets (as a model product) produced by local Saudi pharmaceutical companies (F1 and F3) with others manufactured by an Arabian Emirate company (F5), and two other brands of USA companies (F2 and F4) as global generics. F2 represents the proprietary product produced by Bayer (Bayer Aspirin ® ), to which all other brands were compared. Different quality control tests adopted by the United States Pharmacopeia and/or the British Pharmacopeia were applied to the fi...
Bioadhesive ophthalmic inserts were prepared using single polymer, namely: hydroxypropylmethyl ce... more Bioadhesive ophthalmic inserts were prepared using single polymer, namely: hydroxypropylmethyl cellulose (HPMC), sodium carboxymethyl cellulose (NaCMC), and sodium alginate (SA) in 2% concentration or a mixture of two polymers. The prepared inserts were evaluated in vitro for content uniformity, thickness, folding endurance, weight variation, surface pH, swelling behavior, bioadhesion, in vitro residence time, and drug release. Inserts were evaluated in vivo for intraocular pressure (IOP) lowering effect, in vivo ocular irritancy, and precorneal residence time. In vitro release study exhibited extended release for 8 h. Inserts based on NaCMC were superior over other inserts with respect to swelling, bioadhesion and extended release. Adding HPMC or NaCMC to SA and adding NaCMC to HPMC improved the characteristics of SA and HPMC inserts, respectively. All inserts showed a significant IOP lowering in normotensive rabbits. SA based inserts showed a stable IOP lowering effect for 5 h.
There has been an increasing demand for the development of nanocarriers targeting multiple diseas... more There has been an increasing demand for the development of nanocarriers targeting multiple diseases with a broad range of properties. Due to their tiny size, giant surface area and feasible targetability, nanocarriers have optimized efficacy, decreased side effects and improved stability over conventional drug dosage forms. There are diverse types of nanocarriers that have been synthesized for drug delivery, including dendrimers, liposomes, solid lipid nanoparticles, polymersomes, polymer–drug conjugates, polymeric nanoparticles, peptide nanoparticles, micelles, nanoemulsions, nanospheres, nanocapsules, nanoshells, carbon nanotubes and gold nanoparticles, etc. Several characterization techniques have been proposed and used over the past few decades to control and predict the behavior of nanocarriers both in vitro and in vivo. In this review, we describe some fundamental in vitro, ex vivo, in situ and in vivo characterization methods for most nanocarriers, emphasizing their advantage...
INTRODUCTION: Free palatal and sub-epithelial connective tissue grafts are the most commonly used... more INTRODUCTION: Free palatal and sub-epithelial connective tissue grafts are the most commonly used grafts in periodontal plastic surgeries. The surgical technique of free palatal grafting requires harvesting of soft tissue from the palatal donor site and transplantation to an intraoral recipient one. Post-surgical complications and atypical healing processes have been described in the literature. In order to reduce the morbidity associated with mucogingival surgery, there are several ways to manage the donor site after soft tissue harvesting. Various topically applied formulas and hemostatic agents have been employed to manage post-operative healing at the donor site. OBJECTIVES: to assess the effects of Calendula based topical formula on palatal wound healing after free palatal graft surgery in comparison to oxidized regenerated cellulose. MATERIAL AND METHODS This randomized, controlled trial included twenty-four surgical sites for palatal graft procurement, divided equally into tw...
Natural pharmaceutical excipients have been applied extensively in the past decades owing to thei... more Natural pharmaceutical excipients have been applied extensively in the past decades owing to their safety and biocompatibility. Zein, a natural protein of plant origin offers great benefit over other synthetic polymers used in controlled drug and biomedical delivery systems. It was used in a variety of medical fields including pharmaceutical and biomedical drug targeting, vaccine, tissue engineering, and gene delivery. Being biodegradable and biocompatible, the current review focuses on the history and the medical application of zein as an attractive still promising biopolymer. Areas covered: The current review gives a broadscope on zein as a still promising protein excipient in different fields. Zein- based drug and biomedical delivery systems are discussed with special focus on current and potential application in controlled drug delivery systems, and tissue engineering. Expert opinion: Zein as a protein of natural origin can still be considered a promising polymer in the field of...
International Journal of Pharmacy and Pharmaceutical Sciences
Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance ... more Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs. Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients. Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.
International Journal of Pharmacy and Pharmaceutical Sciences
Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance ... more Objective: Development of sublingual fast dissolving lyophilized almotriptan tablets, to enhance its pre-gastric absorption and so alleviating the gastrointestinal dysmotility that is commonly associated with migraineurs. Methods: Primary almotriptan lyophilized tablets (Alm-lyotab), were prepared using polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), gelatin, or sodium alginate, as a bulk forming agent and mannitol as a disintegrant, cryoprotectant and taste improver. Physical properties, wetting time, in vitro dissolution and disintegration behaviour, were investigated. A combination of PVP, gelatin and chitosan in different ratios with mannitol were developed and characterised for further improvement. Optimised formula was examined by scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). Results: Both PVP and gelatin primary formulations showed elegant appearance with fast in vitro disintegration time of 5.67 and 5.64 sec, short wetting time of 4.06 and 4.05 sec, respectively, and high in vitro release rate of about 80% after 1 min, thus they were selected for further improvement. Optimised formula from polymer blend formulations (F8) which consisted of PVP: gelatin: chitosan in a ratio of its constituting solutions of 1:5:0.5, exhibited an elegant appearance, drug content of 98.75 %, in vivo disintegration time of 1.85 sec and complete drug release within 1 min. SEM micrographs revealed spongy, highly porous structure. DSC results indicated the presence of the drug in its crystalline form. FTIR studies revealed no interaction between the drug and excipients. Conclusion: Sublingual instantly dissolving Almo-lyotab was successfully developed and may constitute an advance in the management of acute migraine attacks.
Oral candidiasis may be manifested in the oral cavity as either mild or severe oral fungal infect... more Oral candidiasis may be manifested in the oral cavity as either mild or severe oral fungal infection. This infection results from the overgrowth of Candida species normally existing in the oral cavity in minute amounts based on many predisposing factors. Several aspects have spurred the search for new strategies in the treatment of oral candidiasis, among which are the limited numbers of new antifungal drugs developed in recent years. Previous studies have shown that thyme and clove oils have antimycotic activities and have suggested their incorporation into pharmaceutical preparations. This study aimed to investigate the possibility of the incorporation and characterization of essential oils or their extracted active ingredients in Orabase formulations. Orabase loaded with clove oil, thyme oil, eugenol, and thymol were prepared and evaluated for their antifungal activities, pH, viscosity, erosion and water uptake characteristics, mechanical properties, in vitro release behavior, and ex vivo mucoadhesion properties. All prepared bases showed considerable antifungal activity and acceptable physical characteristics. The release pattern from loaded bases was considerably slow for all oils and active ingredients. All bases showed appreciable adhesion in the in vitro and ex vivo studies. The incorporation of essential oils in Orabase could help in future drug delivery design, with promising outcomes on patients' well-being.
Periodontitis is one of the most important chronic inflammatory dental diseases arising from the ... more Periodontitis is one of the most important chronic inflammatory dental diseases arising from the destructive actions caused by a variety of pathogenic organisms presented in the oral cavity. The aim of this study is the preparation and in vitro evaluation of films for the local treatment of periodontal pockets. The prepared films contained either metronidazole (Mtr), for its antimicrobial effect in periodontal diseases, using a mixture of polymers namely hydroxypropyl methyl cellulose, Carbopol 934 or locally applied Pentoxifylline (PTX), for its anti-inflammatory activity, using chitosan. All films were prepared using solvent casting technique and were evaluated for their physical characteristics, drug content uniformity, surface pH, swelling behavior, mechanical properties and in vitro release. Further characterization was done on the selected formulations using differential scanning calorimetry and scanning electron microscopy for surface structure. Clinical evaluation tests were also performed. Appropriate physical characteristics and mechanical properties for most formulations and their suitability for periodontal application were observed. In vitro drug release from most films showed a burst release rate for both Mtr and PTX during the first 2 h after which the release rate was markedly decreased. Clinical trials on patients revealed the advantageous use of Mtr and PTX as an adjunct treatment with traditionally used dental techniques. The effectiveness of the co-therapy of either drug could add benefit in the eradication of chronic periodontal hazards.
Abstract The aim of this study was to formulate Pentoxyfylline drug (PTX) as a local bioadhesive ... more Abstract The aim of this study was to formulate Pentoxyfylline drug (PTX) as a local bioadhesive Carbopol (Cbp) based gels for the aid of bone induction around an endosseus oral implant. The local delivery of the drug will probably avoid most of the problems associated with its systemic use including; disturbances in gastrointestinal tract and the central nervous system. Two concentrations of 1% and 3% Cbp containing 1% PTX were prepared. The gels were investigated for their physicochemical properties. Cbp based gels were found to be translucent with good homogeneity, uniform distribution of the drug and absence of any lumps. The pH of the gels was within neutrality, 7.1, which is considered to be acceptable to avoid the risk of any possible irritation in the oral cavity. The Cbp gels exhibited satisfactory bioadhesive properties and a pseudo-plastic rheological behavior. Cumulative drug released from the gels showed a controlled-release for more than 24 hours with the order of 3% >1% and the drug was released by diffusion mechanism from both gels. Statistical analysis revealed non-significant difference in drug content, rheological property and release rate of the stored gels for six months compared to the fresh ones. In vivo experimental results in rabbits have shown significant difference in bone depth induction of 3% and 1% Cbp gels with the formation of strong organized bone over the control group. Local administration of Pentoxifylline could be regarded as a valid approach in the management of osseointegration.
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