Benznidazole, the first line drug for Chagas disease treatment, presents a low solubility, limiti... more Benznidazole, the first line drug for Chagas disease treatment, presents a low solubility, limiting the possibilities for its formulation. In this work, solid dispersions´ technology was exploited to increase benznidazole kinetic solubility and dissolution rate, seeking for an improvement in its bioperformance. A physical mixture (PM) and a solid dispersion (SD) using Poloxamer 407 as carrier were prepared and characterized. Dissolution tests were performed and data were analyzed with the lumped model, which allowed to calculate different parameters of pharmaceutical relevance. A bioactivity assay was also carried out to probe the SD anti-trypanocidal activity. Among the most relevant results, the initial dissolution rate of the benznidazole SD was near 3, 4 and about 400-fold faster than the PM, a commercial formulation (CF) and an extracted benznidazole, respectivley. The times needed for an 80% of drug dissolution were 3.6 (SD), 46.4 (PM), and 238.7 min (CF); while the dissolutio...
Purpose: To investigate the hematinic, anti-plasmodial potentials, and toxic effects of an aqueou... more Purpose: To investigate the hematinic, anti-plasmodial potentials, and toxic effects of an aqueous extract of the leaf of Justicia secunda in mice (Mus musculus) made anemic by Plasmodium beighei. Methods: The LD50 of J. secunda was determined using Lorke’s method. Male albino mice ages 4 – 5 months, totaling forty-eight (48), were assigned at random to six groups (1 – 6). Groups 1, 2, and 3 mice were P. berghei-infected and were given extract doses of 200, 400, and 600 mg/kg of body weight, respectively. Group 4 (positive control) was infected and treated with 0.3 mL of vitamin B12 (standard). Group 5 (negative control) was infected and untreated, while group 6 (normal control) was uninfected and untreated. Blood samples were taken on days 7, 12, and 16 post-infections to measure haemoglobin (Hb), red blood cells (RBC), packed cell volume (PCV), alanine transaminase, aspartate transaminase, alkaline phosphatase, creatinine, and urea using standard methods. Results: Lower concentrat...
Quinine (QHCl) as an antimalarial drug has remained very relevant 400 years after its effectivene... more Quinine (QHCl) as an antimalarial drug has remained very relevant 400 years after its effectiveness was discovered. Unlike other antimalarials, the development of resistance to quinine has been slow. Hence, this drug is till date still used for the treatment of severe and cerebral malaria, for malaria treatment in all trimesters of pregnancy, and in combination with doxycycline against multi-drug resistant parasites. The declined in its administration over the years is mainly associated with poor tolerability due to its gastrointestinal (GIT) side effects such as cinchonism, complex dosing regimen and bitter taste, all of which result in poor compliance. Hence our research was aimed at redesigning quinine using nanotechnology and investigating an alternative route for its administration for the treatment of malaria. A nanosuspension (NS) of QHCl was formulated to suit intranasal administration. QHCl-NS was prepared using lipid matrices made up of solidified reverse micellar solution...
The outbreak of the COVID-19 pandemic in 2019 has been one of the greatest challenges modern medi... more The outbreak of the COVID-19 pandemic in 2019 has been one of the greatest challenges modern medicine and science has ever faced. It has affected millions of people around the world and altered human life and activities as we once knew. The high prevalence as well as an extended period of incubations which usually does not present with symptoms have played a formidable role in the transmission and infection of millions. A lot of research has been carried out on developing suitable treatment and effective preventive measures for the control of the pandemic. Preventive strategies which include social distancing, use of masks, washing of hands, and contact tracing have been effective in slowing the spread of the virus; however, the infectious nature of the SARS-COV-2 has made these strategies unable to eradicate its spread. In addition, the continuous increase in the number of cases and death, as well as the appearance of several variants of the virus, has necessitated the development of effective and safe vaccines in a bid to ensure that human activities can return to normalcy. Nanotechnology has been of great benefit in the design of vaccines as nano-sized materials have been known to aid the safe and effective delivery of antigens as well as serve as suitable adjuvants to potentiate responses to vaccines. There are only four vaccine candidates currently approved for use in humans while many other candidates are at various levels of development. This review seeks to provide updated information on the current nano-technological strategies employed in the development of COVID-19 vaccines.
Aim: Anterior eye segment disorders are treated with eye drops and ointments, which have low ocul... more Aim: Anterior eye segment disorders are treated with eye drops and ointments, which have low ocular bioavailability necessitating the need for improved alternatives. Lipid microsuspension of gentamicin sulphate was developed for the treatment of susceptible eye diseases. Materials & methods: Lipid microsuspensions encapsulating gentamicin sulphate were produced by hot homogenization and evaluated. Ex vivo permeation and ocular irritancy tests were also conducted. Results & conclusion: Stable microsuspensions with high entrapment efficiency and satisfactory osmolarities were obtained. Release studies achieved 49–88% in vitro release at 12 h with sustained permeability of gentamicin compared with conventional gentamicin eye drop (Evril®). No irritation was observed following Draize’s test. The microsuspensions have great potential as ocular delivery system of gentamicin sulphate.
Early treatment with parenteral antimalarials is key in preventing deaths and complications assoc... more Early treatment with parenteral antimalarials is key in preventing deaths and complications associated with severe and cerebral malaria. This can be challenging in 'hard-to-reach' areas in Africa where transit time to hospitals with facilities to administer drugs parenterally can be more than 6 h. Consequently, the World Health Organization has recommended the use of artesunate (ATS) suppositories for emergency treatment of patients, however, this treatment is only for children under 6 years. The intranasal route (INR) can provide a safe and effective alternative to parenteral and rectal routes for patients of all ages; thus, reducing delays to the initiation of treatment. Hence, we designed ATS-loaded nanostructured lipid carriers (NLCs) for intranasal administration. ATS-NLCs were formulated using varying concentrations of lipid matrices made up of solidified reverse micellar solutions (SRMS) comprising a 1:2 ratio of Phospholipon ® 90H and lipids (Softisan ® 154 or Compritol ®). ATS-NLCs were spherical, and the small sizes of ATS-NLCs obtained for some formulations (76.56 ± 1.04 nm) is an indication that ATS-NLCs can pass through the nasal mucosa and reach the brain or systemic circulation. Encapsulation efficiency of ATS in NLCs was ≥70% for all formulations. ATS-NLCs achieved up to 40% in vitro drug release in 1 h, while ex vivo permeation studies revealed that formulating ATS as NLCs enhanced permeation through pig nasal mucosa better than drug solution. Most importantly, the activity and reduction in parasitaemia [in mice infected with plasmodium berghei ANKA in a murine cerebral malaria model] by ATS-NLCs administered through the INR (54.70%, 33.28%) was comparable to intramuscular administration (58.80%, 42.18%), respectively. Therefore, intranasal administration of NLCs of ATS has great potentials to serve as a satisfactory alternative to parenteral administration for the treatment of severe and cerebral malaria in both adults and children in remote areas of sub-Saharan Africa.
Malaria, a leading cause of mortality and morbidity in the developing world, with children aged u... more Malaria, a leading cause of mortality and morbidity in the developing world, with children aged under 5 years, accounts for 61% of all the global malaria deaths. The World Health Organization approved fixed-dose first-line artemisinin-based combination therapy (ACT) – artemether-lumefantrine for effective malaria treatment, is challenged by poor aqueous solubility and inadequate bioavailability leading to treatment failures and emergence of resistant strains. This study focuses on evaluating novel lumefantrine (LF) polymethacrylate-urea solid solutions comprising of a retarding polymer for enhanced anti-plasmodial efficacy comparable with existing artemether-lumefantrine combination therapy. Lumefantrine polymethacrylate-urea solid solutions were prepared by solvent evaporation and characterized by differential scanning calorimetry (DSC), and dissolution studies. In vivo anti-plasmodial activity was determined by measuring the schizonticidal activity of Plasmodium berghei-infected m...
Newbouldia laevis (P. Beauv.) is a tropical rainforest plant used in traditional folk medicine fo... more Newbouldia laevis (P. Beauv.) is a tropical rainforest plant used in traditional folk medicine for the treatment of malaria, cough, joint pains, stomach ache, oedema and inflammation. The main thrust of this research work was to study the analgesic/anti-nociceptive properties of N. laevis-loaded solid lipid microdispersions. N. laevis leaves were extracted using ethanol, and the extract was formulated into solid lipid microdispersions using lipid matrix comprising a rational blend of Precirol® ATO 5 and Softisan® 154. Characterization of the solid lipid microdispersions include determination of morphology, particle size, pH, thermal property, encapsulation efficiency percentage and analgesic/anti-nociceptive property. The results obtained showed that the particles were spherical with sizes ranging from 40 µm to 125 µm. The solid lipid microdispersions maintained a stable pH within the acidic region of 5–6 with insignificant variations ( p > 0.05) over a period of 90 days. Thermal...
Poor aqueous solubility of artemether and lumefantrine makes it important to seek better ways of ... more Poor aqueous solubility of artemether and lumefantrine makes it important to seek better ways of enhancing their oral delivery and bioavailability. To formulate and carry out in vitro and anti-malarial pharmacodynamic evaluations of solidified reverse micellar solutions (SRMS)-based solid lipid microparticles (SLMs) of artemether and lumefantrine for oral delivery and improved bioavailability. Rational blends of Softisan(®)154 and Phospholipon(®)90H lipid matrices, and different concentrations of artemether and lumefantrine were used to formulate several batches of SLMs. Drug-free SLMs were also formulated. Morphology, particle size, encapsulation efficiency (EE%) and pH studies were performed. In vitro release studies were performed in alcoholic buffer, simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) without enzymes. Anti-malarial pharmacodynamic studies were conducted in mice. Stable, smooth and spherical particles with sizes ranging from 4.2 ± 0.02 to 9.3 ± 0.8 µm were formed. EE% of 92.2-97.3% and 30.2-84.7% and pH of 3.0 ± 0.02 to 4.9 ± 0.12 and 3.0 ± 0.02 to 5.8 ± 0.05 were obtained for artemether and lumefantrine SLMs, respectively. Release of 100, 88.28 and 75.49%, as well as 63.26, 34.31 and 56.17% were recorded for artemether and lumefantrine in alcoholic buffer, SGF and SIF, respectively. Pharmacodynamic studies indicated very significant (p < 0.05) clearance of parasitaemia in plasmodium-infected mice by the drug-loaded SLMs. Oral delivery and bioavailability of artemether and lumefantrine could be improved using SRMS-based SLMs.
Surface modified self-nanoemulsifying formulations (SNEFs) loaded with gentamicin were formulated... more Surface modified self-nanoemulsifying formulations (SNEFs) loaded with gentamicin were formulated using suitable blends of soybean oil, a mixture of Kolliphor
Albizia adianthifolia (commonly known as flat crown albizia) is a leguminous plant of the family ... more Albizia adianthifolia (commonly known as flat crown albizia) is a leguminous plant of the family Fabaceae. A. adianthifolia roots were extracted with methanol and the extract thereafter fractionated to afford the chloroform fraction. The root extract and the fraction were screened for their antimicrobial potential against clinical strains of Candida spps viz: Candida albicans and Candida krusei using agar diffusion method. Fluconazole and ticonazole were used as reference drugs. Combined activity of the plant extract or fraction with the reference drugs was done using the agar dilution Checker board method. Acute toxicity study and preliminary phytochemical analysis were carried out on the plant samples. The results obtained showed that the minimum inhibitory concentrations (MIC) of fluconazole/ticonazole ranges from 1.96 to 5.90 µg/ml while the MIC of the A. adianthifolia root extract/fraction ranges from 5.49 to 12.59 mg/ml against the test organisms. Synergy was predominantly observed in the interaction against Candida species. The median acute toxicity value (LD50) of the methanol extract and chloro- form fraction were determined to be greater than 5000 mg/kg body weight in each case. Phytochemical screening revealed the presence of alkaloids, flavonoids, tannins, glycosides. It was concluded that the extract of A. adianthifolia and its chloroform fraction posses antimicrobial activity hence justifying the ethnomedical uses of the plant in the treatment of fungal infections. The combination of the extract and flucona- zole or ticonazole produces synergism predominantly also indicating the potentials of combining the extract of the plant and the standard drugs for the treatment of candida infections.
Malaria - Recent Advances, and New Perspectives [Working Title]
This chapter X-rayed antimalarial drug resistance (ADR) by plasmodium species with a particular f... more This chapter X-rayed antimalarial drug resistance (ADR) by plasmodium species with a particular focus on P. falciparum, which is the most deadly species of the malaria parasite responsible for over 90% of the global malaria burden domiciled in Sub-Saharan Africa. The introduction intently looked at malaria therapeutics across the decades and the development of drug resistance by the parasite. With the malaria parasite (P. falciparum) as the focal point, the mechanisms by which they develop resistance to antimalarial drugs was looked at, including factors affecting drug resistance development. Armed with this knowledge, the chapter also highlighted the therapeutic interventions taken against this hydra-headed monster together with their limitations and recent advances towards addressing those limitations or opening new frontiers for research exploration. Future perspectives that will provide research strategy and direction as possible tools for combating drug resistance development b...
Oral delivery of insulin provides a good alternative because it is non-invasive and patient-frien... more Oral delivery of insulin provides a good alternative because it is non-invasive and patient-friendly. However, multiple challenges affected this route. To overcome barriers for oral delivery of insulin, we aimed to develop a novel insulin-loaded microemulsion system based on snail mucin for oral administration. The strategy in the novel system of using mucin loading insulin into the inner core of prepared water in oil microemulsion to provide sustained released, increased in vivo stability and enhanced drug absorption in the gastrointestinal tract. We report how microemulsion composed of varying ratios of snail mucin and Tween® 80 (1:9-9:1) using oil/water emulsion preparation method influenced insulin performance after oral administration. The results obtained include an encapsulation efficiency of above 70 %; in vitro release was sustained over 10 h and in vivo evaluations in diabetic rat model shows that insulin-loaded microencapsulation effectively reduced blood glucose levels over a period >8 h after oral administration. Therefore, we suggest that the developed formulation for oral insulin can be a promising alternative dosage form for oral protein delivery.
Benznidazole, the first line drug for Chagas disease treatment, presents a low solubility, limiti... more Benznidazole, the first line drug for Chagas disease treatment, presents a low solubility, limiting the possibilities for its formulation. In this work, solid dispersions´ technology was exploited to increase benznidazole kinetic solubility and dissolution rate, seeking for an improvement in its bioperformance. A physical mixture (PM) and a solid dispersion (SD) using Poloxamer 407 as carrier were prepared and characterized. Dissolution tests were performed and data were analyzed with the lumped model, which allowed to calculate different parameters of pharmaceutical relevance. A bioactivity assay was also carried out to probe the SD anti-trypanocidal activity. Among the most relevant results, the initial dissolution rate of the benznidazole SD was near 3, 4 and about 400-fold faster than the PM, a commercial formulation (CF) and an extracted benznidazole, respectivley. The times needed for an 80% of drug dissolution were 3.6 (SD), 46.4 (PM), and 238.7 min (CF); while the dissolutio...
Purpose: To investigate the hematinic, anti-plasmodial potentials, and toxic effects of an aqueou... more Purpose: To investigate the hematinic, anti-plasmodial potentials, and toxic effects of an aqueous extract of the leaf of Justicia secunda in mice (Mus musculus) made anemic by Plasmodium beighei. Methods: The LD50 of J. secunda was determined using Lorke’s method. Male albino mice ages 4 – 5 months, totaling forty-eight (48), were assigned at random to six groups (1 – 6). Groups 1, 2, and 3 mice were P. berghei-infected and were given extract doses of 200, 400, and 600 mg/kg of body weight, respectively. Group 4 (positive control) was infected and treated with 0.3 mL of vitamin B12 (standard). Group 5 (negative control) was infected and untreated, while group 6 (normal control) was uninfected and untreated. Blood samples were taken on days 7, 12, and 16 post-infections to measure haemoglobin (Hb), red blood cells (RBC), packed cell volume (PCV), alanine transaminase, aspartate transaminase, alkaline phosphatase, creatinine, and urea using standard methods. Results: Lower concentrat...
Quinine (QHCl) as an antimalarial drug has remained very relevant 400 years after its effectivene... more Quinine (QHCl) as an antimalarial drug has remained very relevant 400 years after its effectiveness was discovered. Unlike other antimalarials, the development of resistance to quinine has been slow. Hence, this drug is till date still used for the treatment of severe and cerebral malaria, for malaria treatment in all trimesters of pregnancy, and in combination with doxycycline against multi-drug resistant parasites. The declined in its administration over the years is mainly associated with poor tolerability due to its gastrointestinal (GIT) side effects such as cinchonism, complex dosing regimen and bitter taste, all of which result in poor compliance. Hence our research was aimed at redesigning quinine using nanotechnology and investigating an alternative route for its administration for the treatment of malaria. A nanosuspension (NS) of QHCl was formulated to suit intranasal administration. QHCl-NS was prepared using lipid matrices made up of solidified reverse micellar solution...
The outbreak of the COVID-19 pandemic in 2019 has been one of the greatest challenges modern medi... more The outbreak of the COVID-19 pandemic in 2019 has been one of the greatest challenges modern medicine and science has ever faced. It has affected millions of people around the world and altered human life and activities as we once knew. The high prevalence as well as an extended period of incubations which usually does not present with symptoms have played a formidable role in the transmission and infection of millions. A lot of research has been carried out on developing suitable treatment and effective preventive measures for the control of the pandemic. Preventive strategies which include social distancing, use of masks, washing of hands, and contact tracing have been effective in slowing the spread of the virus; however, the infectious nature of the SARS-COV-2 has made these strategies unable to eradicate its spread. In addition, the continuous increase in the number of cases and death, as well as the appearance of several variants of the virus, has necessitated the development of effective and safe vaccines in a bid to ensure that human activities can return to normalcy. Nanotechnology has been of great benefit in the design of vaccines as nano-sized materials have been known to aid the safe and effective delivery of antigens as well as serve as suitable adjuvants to potentiate responses to vaccines. There are only four vaccine candidates currently approved for use in humans while many other candidates are at various levels of development. This review seeks to provide updated information on the current nano-technological strategies employed in the development of COVID-19 vaccines.
Aim: Anterior eye segment disorders are treated with eye drops and ointments, which have low ocul... more Aim: Anterior eye segment disorders are treated with eye drops and ointments, which have low ocular bioavailability necessitating the need for improved alternatives. Lipid microsuspension of gentamicin sulphate was developed for the treatment of susceptible eye diseases. Materials & methods: Lipid microsuspensions encapsulating gentamicin sulphate were produced by hot homogenization and evaluated. Ex vivo permeation and ocular irritancy tests were also conducted. Results & conclusion: Stable microsuspensions with high entrapment efficiency and satisfactory osmolarities were obtained. Release studies achieved 49–88% in vitro release at 12 h with sustained permeability of gentamicin compared with conventional gentamicin eye drop (Evril®). No irritation was observed following Draize’s test. The microsuspensions have great potential as ocular delivery system of gentamicin sulphate.
Early treatment with parenteral antimalarials is key in preventing deaths and complications assoc... more Early treatment with parenteral antimalarials is key in preventing deaths and complications associated with severe and cerebral malaria. This can be challenging in 'hard-to-reach' areas in Africa where transit time to hospitals with facilities to administer drugs parenterally can be more than 6 h. Consequently, the World Health Organization has recommended the use of artesunate (ATS) suppositories for emergency treatment of patients, however, this treatment is only for children under 6 years. The intranasal route (INR) can provide a safe and effective alternative to parenteral and rectal routes for patients of all ages; thus, reducing delays to the initiation of treatment. Hence, we designed ATS-loaded nanostructured lipid carriers (NLCs) for intranasal administration. ATS-NLCs were formulated using varying concentrations of lipid matrices made up of solidified reverse micellar solutions (SRMS) comprising a 1:2 ratio of Phospholipon ® 90H and lipids (Softisan ® 154 or Compritol ®). ATS-NLCs were spherical, and the small sizes of ATS-NLCs obtained for some formulations (76.56 ± 1.04 nm) is an indication that ATS-NLCs can pass through the nasal mucosa and reach the brain or systemic circulation. Encapsulation efficiency of ATS in NLCs was ≥70% for all formulations. ATS-NLCs achieved up to 40% in vitro drug release in 1 h, while ex vivo permeation studies revealed that formulating ATS as NLCs enhanced permeation through pig nasal mucosa better than drug solution. Most importantly, the activity and reduction in parasitaemia [in mice infected with plasmodium berghei ANKA in a murine cerebral malaria model] by ATS-NLCs administered through the INR (54.70%, 33.28%) was comparable to intramuscular administration (58.80%, 42.18%), respectively. Therefore, intranasal administration of NLCs of ATS has great potentials to serve as a satisfactory alternative to parenteral administration for the treatment of severe and cerebral malaria in both adults and children in remote areas of sub-Saharan Africa.
Malaria, a leading cause of mortality and morbidity in the developing world, with children aged u... more Malaria, a leading cause of mortality and morbidity in the developing world, with children aged under 5 years, accounts for 61% of all the global malaria deaths. The World Health Organization approved fixed-dose first-line artemisinin-based combination therapy (ACT) – artemether-lumefantrine for effective malaria treatment, is challenged by poor aqueous solubility and inadequate bioavailability leading to treatment failures and emergence of resistant strains. This study focuses on evaluating novel lumefantrine (LF) polymethacrylate-urea solid solutions comprising of a retarding polymer for enhanced anti-plasmodial efficacy comparable with existing artemether-lumefantrine combination therapy. Lumefantrine polymethacrylate-urea solid solutions were prepared by solvent evaporation and characterized by differential scanning calorimetry (DSC), and dissolution studies. In vivo anti-plasmodial activity was determined by measuring the schizonticidal activity of Plasmodium berghei-infected m...
Newbouldia laevis (P. Beauv.) is a tropical rainforest plant used in traditional folk medicine fo... more Newbouldia laevis (P. Beauv.) is a tropical rainforest plant used in traditional folk medicine for the treatment of malaria, cough, joint pains, stomach ache, oedema and inflammation. The main thrust of this research work was to study the analgesic/anti-nociceptive properties of N. laevis-loaded solid lipid microdispersions. N. laevis leaves were extracted using ethanol, and the extract was formulated into solid lipid microdispersions using lipid matrix comprising a rational blend of Precirol® ATO 5 and Softisan® 154. Characterization of the solid lipid microdispersions include determination of morphology, particle size, pH, thermal property, encapsulation efficiency percentage and analgesic/anti-nociceptive property. The results obtained showed that the particles were spherical with sizes ranging from 40 µm to 125 µm. The solid lipid microdispersions maintained a stable pH within the acidic region of 5–6 with insignificant variations ( p > 0.05) over a period of 90 days. Thermal...
Poor aqueous solubility of artemether and lumefantrine makes it important to seek better ways of ... more Poor aqueous solubility of artemether and lumefantrine makes it important to seek better ways of enhancing their oral delivery and bioavailability. To formulate and carry out in vitro and anti-malarial pharmacodynamic evaluations of solidified reverse micellar solutions (SRMS)-based solid lipid microparticles (SLMs) of artemether and lumefantrine for oral delivery and improved bioavailability. Rational blends of Softisan(®)154 and Phospholipon(®)90H lipid matrices, and different concentrations of artemether and lumefantrine were used to formulate several batches of SLMs. Drug-free SLMs were also formulated. Morphology, particle size, encapsulation efficiency (EE%) and pH studies were performed. In vitro release studies were performed in alcoholic buffer, simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) without enzymes. Anti-malarial pharmacodynamic studies were conducted in mice. Stable, smooth and spherical particles with sizes ranging from 4.2 ± 0.02 to 9.3 ± 0.8 µm were formed. EE% of 92.2-97.3% and 30.2-84.7% and pH of 3.0 ± 0.02 to 4.9 ± 0.12 and 3.0 ± 0.02 to 5.8 ± 0.05 were obtained for artemether and lumefantrine SLMs, respectively. Release of 100, 88.28 and 75.49%, as well as 63.26, 34.31 and 56.17% were recorded for artemether and lumefantrine in alcoholic buffer, SGF and SIF, respectively. Pharmacodynamic studies indicated very significant (p < 0.05) clearance of parasitaemia in plasmodium-infected mice by the drug-loaded SLMs. Oral delivery and bioavailability of artemether and lumefantrine could be improved using SRMS-based SLMs.
Surface modified self-nanoemulsifying formulations (SNEFs) loaded with gentamicin were formulated... more Surface modified self-nanoemulsifying formulations (SNEFs) loaded with gentamicin were formulated using suitable blends of soybean oil, a mixture of Kolliphor
Albizia adianthifolia (commonly known as flat crown albizia) is a leguminous plant of the family ... more Albizia adianthifolia (commonly known as flat crown albizia) is a leguminous plant of the family Fabaceae. A. adianthifolia roots were extracted with methanol and the extract thereafter fractionated to afford the chloroform fraction. The root extract and the fraction were screened for their antimicrobial potential against clinical strains of Candida spps viz: Candida albicans and Candida krusei using agar diffusion method. Fluconazole and ticonazole were used as reference drugs. Combined activity of the plant extract or fraction with the reference drugs was done using the agar dilution Checker board method. Acute toxicity study and preliminary phytochemical analysis were carried out on the plant samples. The results obtained showed that the minimum inhibitory concentrations (MIC) of fluconazole/ticonazole ranges from 1.96 to 5.90 µg/ml while the MIC of the A. adianthifolia root extract/fraction ranges from 5.49 to 12.59 mg/ml against the test organisms. Synergy was predominantly observed in the interaction against Candida species. The median acute toxicity value (LD50) of the methanol extract and chloro- form fraction were determined to be greater than 5000 mg/kg body weight in each case. Phytochemical screening revealed the presence of alkaloids, flavonoids, tannins, glycosides. It was concluded that the extract of A. adianthifolia and its chloroform fraction posses antimicrobial activity hence justifying the ethnomedical uses of the plant in the treatment of fungal infections. The combination of the extract and flucona- zole or ticonazole produces synergism predominantly also indicating the potentials of combining the extract of the plant and the standard drugs for the treatment of candida infections.
Malaria - Recent Advances, and New Perspectives [Working Title]
This chapter X-rayed antimalarial drug resistance (ADR) by plasmodium species with a particular f... more This chapter X-rayed antimalarial drug resistance (ADR) by plasmodium species with a particular focus on P. falciparum, which is the most deadly species of the malaria parasite responsible for over 90% of the global malaria burden domiciled in Sub-Saharan Africa. The introduction intently looked at malaria therapeutics across the decades and the development of drug resistance by the parasite. With the malaria parasite (P. falciparum) as the focal point, the mechanisms by which they develop resistance to antimalarial drugs was looked at, including factors affecting drug resistance development. Armed with this knowledge, the chapter also highlighted the therapeutic interventions taken against this hydra-headed monster together with their limitations and recent advances towards addressing those limitations or opening new frontiers for research exploration. Future perspectives that will provide research strategy and direction as possible tools for combating drug resistance development b...
Oral delivery of insulin provides a good alternative because it is non-invasive and patient-frien... more Oral delivery of insulin provides a good alternative because it is non-invasive and patient-friendly. However, multiple challenges affected this route. To overcome barriers for oral delivery of insulin, we aimed to develop a novel insulin-loaded microemulsion system based on snail mucin for oral administration. The strategy in the novel system of using mucin loading insulin into the inner core of prepared water in oil microemulsion to provide sustained released, increased in vivo stability and enhanced drug absorption in the gastrointestinal tract. We report how microemulsion composed of varying ratios of snail mucin and Tween® 80 (1:9-9:1) using oil/water emulsion preparation method influenced insulin performance after oral administration. The results obtained include an encapsulation efficiency of above 70 %; in vitro release was sustained over 10 h and in vivo evaluations in diabetic rat model shows that insulin-loaded microencapsulation effectively reduced blood glucose levels over a period >8 h after oral administration. Therefore, we suggest that the developed formulation for oral insulin can be a promising alternative dosage form for oral protein delivery.
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