The solubility and dissolution rate of Lovastatin, a drug used for the treatment of hyperlipidaemia. Lovastatin is a selective competitive inhibitor of HMG Co-A reductase. However, its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. The present investigations showed that solubility of Lovastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Lovastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of Lovastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.
{"title":"Formulation and Development of Solid Dispersion System for Enhancement of Solubility and Dissolution Rate of Lovastatin","authors":"Ashutosh Kumar Upadhyay, Naveen Gupta, Neeraj Sharma, Dharmendra S. Rajput, Ankita Shukla","doi":"10.52711/0975-4377.2023.00028","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00028","url":null,"abstract":"The solubility and dissolution rate of Lovastatin, a drug used for the treatment of hyperlipidaemia. Lovastatin is a selective competitive inhibitor of HMG Co-A reductase. However, its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. The present investigations showed that solubility of Lovastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Lovastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of Lovastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136083315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00018
Nausaba Moazzam, Naveen Gupta, N. Sharma, Dharmendra S. Rajput, Ankita Shukla
Mucoadhesive thermo reversible in-situ nasal gel of Meperidine HCl was designed and developed to sustain its release due to the increased nasal residence time of the formulation. Poloxamer 407 (PF 127) was selected as it has excellent thermo sensitive gelling properties. HPMCK4M was added to impart mucoadhesive to the formulation, and PEG 400 was used to enhance the drug release. 32 Factorial designs were employed to assess the effect of concentration of HPMCK4M and PEG 400 on the performance of in-situ nasal gel systematically and to optimize the formulation. Meperidine Hydrochloride is a centrally acting analgesic. It has 33% bioavailability due to its first pass effect and hence possesses problems in the development of oral sustained release formulations. An optimized in-situ nasal gel was evaluated for appearance, pH, drug content, gelation temperature, mucoadhesive force, viscosity and ex-vivo permeability of drug through nasal mucosa of a goat. Additionally, this formulation was proved to be safe as histopathological studies revealed no deleterious effect on nasal mucosa of a goat after prolonged exposure of 21 days to the optimized formulation. Thus the release of Meperidine Hydrochloride can be sustained if formulated in an in-situ nasal gel containing poloxamer 407 to achieve its prolonged action.
{"title":"Design, Development and Formulation of Mucoadhesive In-situ Nasal Gel of Meperidine Hydrochloride","authors":"Nausaba Moazzam, Naveen Gupta, N. Sharma, Dharmendra S. Rajput, Ankita Shukla","doi":"10.52711/0975-4377.2023.00018","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00018","url":null,"abstract":"Mucoadhesive thermo reversible in-situ nasal gel of Meperidine HCl was designed and developed to sustain its release due to the increased nasal residence time of the formulation. Poloxamer 407 (PF 127) was selected as it has excellent thermo sensitive gelling properties. HPMCK4M was added to impart mucoadhesive to the formulation, and PEG 400 was used to enhance the drug release. 32 Factorial designs were employed to assess the effect of concentration of HPMCK4M and PEG 400 on the performance of in-situ nasal gel systematically and to optimize the formulation. Meperidine Hydrochloride is a centrally acting analgesic. It has 33% bioavailability due to its first pass effect and hence possesses problems in the development of oral sustained release formulations. An optimized in-situ nasal gel was evaluated for appearance, pH, drug content, gelation temperature, mucoadhesive force, viscosity and ex-vivo permeability of drug through nasal mucosa of a goat. Additionally, this formulation was proved to be safe as histopathological studies revealed no deleterious effect on nasal mucosa of a goat after prolonged exposure of 21 days to the optimized formulation. Thus the release of Meperidine Hydrochloride can be sustained if formulated in an in-situ nasal gel containing poloxamer 407 to achieve its prolonged action.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75527306","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00013
Laxman S Vijapur, Anita R. Desai, Gajanand G. Satbhai, Supriya P. Suragond, Bhagyashree V S, Farha Hassan
The study aimed to formulate a herbal shampoo and evaluate its physicochemical properties. The herbal shampoo was formulated by adding the extracts of amla, bhringraj, curry leaves, reetha and shikakaiin different proportions to water, methyl paraben was added and completely dissolved. To this 2% of carbopol-934 was added to form a gel. All extracts were weighed and dissolved to form a homogenous solution, lemon juice and citric acid was stirred properly with it. The evaluation parameters such as visual inspection, foaming ability, foaming stability, pH, dirt dispersion, measurement of surface tension, rheological evaluation and percentage of solid contents were performed to determine the physicochemical properties of formulated herbal shampoo. The formulated herbal shampoo was also evaluated for conditioning performance by administering a blind test to 30 student volunteers. It showed low surface tension, good foam stability after 5 min. The results indicated that the formulated shampoo was observed to be suitable for use and safe.
{"title":"Formulation and Evaluation of Conditioning Herbal Shampoo","authors":"Laxman S Vijapur, Anita R. Desai, Gajanand G. Satbhai, Supriya P. Suragond, Bhagyashree V S, Farha Hassan","doi":"10.52711/0975-4377.2023.00013","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00013","url":null,"abstract":"The study aimed to formulate a herbal shampoo and evaluate its physicochemical properties. The herbal shampoo was formulated by adding the extracts of amla, bhringraj, curry leaves, reetha and shikakaiin different proportions to water, methyl paraben was added and completely dissolved. To this 2% of carbopol-934 was added to form a gel. All extracts were weighed and dissolved to form a homogenous solution, lemon juice and citric acid was stirred properly with it. The evaluation parameters such as visual inspection, foaming ability, foaming stability, pH, dirt dispersion, measurement of surface tension, rheological evaluation and percentage of solid contents were performed to determine the physicochemical properties of formulated herbal shampoo. The formulated herbal shampoo was also evaluated for conditioning performance by administering a blind test to 30 student volunteers. It showed low surface tension, good foam stability after 5 min. The results indicated that the formulated shampoo was observed to be suitable for use and safe.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83616163","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00019
Joe Chou, R. Lai, Jason Chou, Shelly Fu, Hsin-Ai Tung
Traditionally, the pilot bioequivalence study is a generalpractice for generic drug development. However, due to its difficulty in differentiating the variation between subject and drug formulation for bioequivalence results. A new instrument called PAMPA Dissolution is proposed in this study to improve the correlation between in vitro and in vivo absorption forbioequivalence study. PAMPA Dissolution allows for the simultaneous measurement of drug dissolution (Cb) and permeation (Pe), two key parameters in oral drug absorption according to the validated equation F (drug absorbed) = Cb*Pe*Area. The use of Parallel Artificial Membrane Permeability Assay (PAMPA) eliminates the concern of subject variation. Biorelevant media further allows this device to simulate in vivo conditions closely. Brand and generic formulations of 40 mg telmisartan tablets were used in various studies to demonstrate the potential of PAMPA Dissolution in generic drug development. Bioequivalence predictions between brand and generic telmisartan from PAMPA Dissolution produced avalue（test/reference）for Cmax of 86.3% and a value for AUC of 91.4%, indicating that PAMPA Dissolution predictions conform with bioequivalence requirements. Other parameters such as stirring at different speeds and phospholipids concentrations for PAMPA are also included for optimal performance of the system. Based on these data, the PAMPA Dissolution system is reproducible, precise, and can therefore be applied in predicting bioequivalence study.
{"title":"Enhancing Bioequivalence Predictions with PAMPA Dissolution Using Formulations of Telmisartan","authors":"Joe Chou, R. Lai, Jason Chou, Shelly Fu, Hsin-Ai Tung","doi":"10.52711/0975-4377.2023.00019","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00019","url":null,"abstract":"Traditionally, the pilot bioequivalence study is a generalpractice for generic drug development. However, due to its difficulty in differentiating the variation between subject and drug formulation for bioequivalence results. A new instrument called PAMPA Dissolution is proposed in this study to improve the correlation between in vitro and in vivo absorption forbioequivalence study. PAMPA Dissolution allows for the simultaneous measurement of drug dissolution (Cb) and permeation (Pe), two key parameters in oral drug absorption according to the validated equation F (drug absorbed) = Cb*Pe*Area. The use of Parallel Artificial Membrane Permeability Assay (PAMPA) eliminates the concern of subject variation. Biorelevant media further allows this device to simulate in vivo conditions closely. Brand and generic formulations of 40 mg telmisartan tablets were used in various studies to demonstrate the potential of PAMPA Dissolution in generic drug development. Bioequivalence predictions between brand and generic telmisartan from PAMPA Dissolution produced avalue（test/reference）for Cmax of 86.3% and a value for AUC of 91.4%, indicating that PAMPA Dissolution predictions conform with bioequivalence requirements. Other parameters such as stirring at different speeds and phospholipids concentrations for PAMPA are also included for optimal performance of the system. Based on these data, the PAMPA Dissolution system is reproducible, precise, and can therefore be applied in predicting bioequivalence study.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78582912","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00017
Komal Nirale, Pallavi Wadaskar, Mukul Rajgure
Nanoformulation plays an essential function in emphasising the efficiency of reaching medications such as chemotherapeutic treatments and phytochemicals, and this significance is becoming increasingly recognised. In the course of this experiment, we focused on increasing the bioavailability of resveratrol lby loading it into nanoparticles. Doing so has the potential to reduce the toxicity that is a side effect of conventional formulation as well as minimise the amount of times a dose needs to be administered. The polymer, in its capacity as a carrier, plays a vital role in transporting the drug over the blood-brain barrier, which may be effective in bringing about the desired therapeutic effect. Piperine, acting as both a bio enhancer and an MAO inhibitor, has the potential to not only boost the effectiveness of resveratrol but also provide an additional mode of action that can be used to treat Parkinson's disease in a manner that is both efficient and effective. Additionally, piperine has the potential to be used in place of MAO-B inhibitors like selegline and rosagline. This provides a boost to the ongoing work on particle size in relation to two different medications and a polymer.
{"title":"Design, Fabrication, and Analysis of Resveratrol and Piperine-Loaded Chitosan Nanoparticles with the Purpose of Providing an Enhanced Parkinson's Disease Treatment","authors":"Komal Nirale, Pallavi Wadaskar, Mukul Rajgure","doi":"10.52711/0975-4377.2023.00017","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00017","url":null,"abstract":"Nanoformulation plays an essential function in emphasising the efficiency of reaching medications such as chemotherapeutic treatments and phytochemicals, and this significance is becoming increasingly recognised. In the course of this experiment, we focused on increasing the bioavailability of resveratrol lby loading it into nanoparticles. Doing so has the potential to reduce the toxicity that is a side effect of conventional formulation as well as minimise the amount of times a dose needs to be administered. The polymer, in its capacity as a carrier, plays a vital role in transporting the drug over the blood-brain barrier, which may be effective in bringing about the desired therapeutic effect. Piperine, acting as both a bio enhancer and an MAO inhibitor, has the potential to not only boost the effectiveness of resveratrol but also provide an additional mode of action that can be used to treat Parkinson's disease in a manner that is both efficient and effective. Additionally, piperine has the potential to be used in place of MAO-B inhibitors like selegline and rosagline. This provides a boost to the ongoing work on particle size in relation to two different medications and a polymer.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82585737","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00024
Girijesh Kumar, Naveen Gupta, N. Sharma, Dharmendra S. Rajput, Ankita Shukla
Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. The solubility and dissolution rate of Simvastatin, a drug used for the treatment of hyperlipidaemia. Simvastatin is a selective competitive inhibitor of HMG Co-A reductase. However its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. The present investigations showed that solubility of Simvastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Simvastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of Simvastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.
{"title":"Formulation for Enhancement of Solubility and Dissolution Rate of Simvastatin using Solid Dispersion","authors":"Girijesh Kumar, Naveen Gupta, N. Sharma, Dharmendra S. Rajput, Ankita Shukla","doi":"10.52711/0975-4377.2023.00024","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00024","url":null,"abstract":"Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. The solubility and dissolution rate of Simvastatin, a drug used for the treatment of hyperlipidaemia. Simvastatin is a selective competitive inhibitor of HMG Co-A reductase. However its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. The present investigations showed that solubility of Simvastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Simvastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of Simvastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80324635","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00016
Pallavi Wadaskar, Komal Nirale, Mukul Rajgure
Liposomes and other novel drug delivery carriers are highly adaptable, allowing for the distribution of a wide range of pharmacological compounds. The antibiotic azithromycin is widely regarded as the most effective treatment for acne. Lower efficacy or higher negative effects have led to decreased use of topical azithromycin. In this study, liposomes have been chosen because it is hypothesised that this may lessen the drug's side effects when used in conjunction with Azithromycin. Traditional herbal therapies have been intensively investigated as alternatives to conventional treatments for many ailments due to the possibility for side effects and antibiotic resistance from conventional pharmaceuticals. Thanks to its antibacterial qualities, green tea is one of the most effective natural therapies for acne. The lipid film hydration method was used to create drug-loaded liposomes, and the optimal component ratios were established. Liposomes were studied for their in-vitro drug release properties and characterised for their vesicle size, shape, encapsulation effectiveness, and drug content. Formulations F1 and F6, which included a 1:1 ratio of fat to cholesterol, showed the highest levels of encapsulation efficiency (69.5% and 66.2%, respectively) and in-vitro drug release (82.5 and 82.2 percent, respectively). Carbopol gel has been modified to include liposomal formulations, and the results have been compared to those of commercially available gels that do not use liposomes. Within 24 hours, the release of azithromycin (90.5%) was greater in the non liposomal marketed gel than in the liposomal gel (77.5% and 74.8%) of green tea. Green tea liposomes used in the formulation had a MIC value that was comparable to that of commercially available, non-liposomal gel. It was discovered that azithromycin was more effective than green tea in killing Micrococcus luteus.
{"title":"Liposomes containing azithromycin and green tea as an anti-acne treatment: Formulation and Characterization","authors":"Pallavi Wadaskar, Komal Nirale, Mukul Rajgure","doi":"10.52711/0975-4377.2023.00016","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00016","url":null,"abstract":"Liposomes and other novel drug delivery carriers are highly adaptable, allowing for the distribution of a wide range of pharmacological compounds. The antibiotic azithromycin is widely regarded as the most effective treatment for acne. Lower efficacy or higher negative effects have led to decreased use of topical azithromycin. In this study, liposomes have been chosen because it is hypothesised that this may lessen the drug's side effects when used in conjunction with Azithromycin. Traditional herbal therapies have been intensively investigated as alternatives to conventional treatments for many ailments due to the possibility for side effects and antibiotic resistance from conventional pharmaceuticals. Thanks to its antibacterial qualities, green tea is one of the most effective natural therapies for acne. The lipid film hydration method was used to create drug-loaded liposomes, and the optimal component ratios were established. Liposomes were studied for their in-vitro drug release properties and characterised for their vesicle size, shape, encapsulation effectiveness, and drug content. Formulations F1 and F6, which included a 1:1 ratio of fat to cholesterol, showed the highest levels of encapsulation efficiency (69.5% and 66.2%, respectively) and in-vitro drug release (82.5 and 82.2 percent, respectively). Carbopol gel has been modified to include liposomal formulations, and the results have been compared to those of commercially available gels that do not use liposomes. Within 24 hours, the release of azithromycin (90.5%) was greater in the non liposomal marketed gel than in the liposomal gel (77.5% and 74.8%) of green tea. Green tea liposomes used in the formulation had a MIC value that was comparable to that of commercially available, non-liposomal gel. It was discovered that azithromycin was more effective than green tea in killing Micrococcus luteus.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90618548","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00022
Sushmita Vishwakarma, Naveen Gupta, N. Sharma, Dharmendra S. Rajput, Ankita Shukla
Tramadol Hydrochloride is a centrally acting analgesic. It has 33% bioavailability due to its first pass effect and hence possesses problems in the development of oral sustained release formulations. Muco-adhesive thermo reversible in-situ nasal gel of Tramadol HCl was designed and developed to sustain its release due to the increased nasal residence time of the formulation. Poloxamer 407(PF 127) was selected as it has excellent thermo sensitive gelling properties. HPMCK4M was added to impart muco-adhesive to the formulation, and PEG 400 was used to enhance the drug release. 32 Factorial designs were employed to assess the effect of concentration of HPMCK4M and PEG 400 on the performance of in-situ nasal gel systematically and to optimize the formulation. An optimized in-situ nasal gel was evaluated for appearance, pH, drug content, gelation temperature, mucoadhesive force, viscosity and ex-vivo permeability of drug through nasal mucosa of a goat. Additionally, this formulation was proved to be safe as histopathological studies revealed no deleterious effect on nasal mucosa of a goat after prolonged exposure of 21 days to the optimized formulation. Thus the release of Tramadol Hydrochloride can be sustained if formulated in an in-situ nasal gel containing poloxamer 407 to achieve its prolonged action.
{"title":"Formulation and Evaluation of Mucoadhesive In-situ Nasal Gel of Tramadol Hydrochloride","authors":"Sushmita Vishwakarma, Naveen Gupta, N. Sharma, Dharmendra S. Rajput, Ankita Shukla","doi":"10.52711/0975-4377.2023.00022","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00022","url":null,"abstract":"Tramadol Hydrochloride is a centrally acting analgesic. It has 33% bioavailability due to its first pass effect and hence possesses problems in the development of oral sustained release formulations. Muco-adhesive thermo reversible in-situ nasal gel of Tramadol HCl was designed and developed to sustain its release due to the increased nasal residence time of the formulation. Poloxamer 407(PF 127) was selected as it has excellent thermo sensitive gelling properties. HPMCK4M was added to impart muco-adhesive to the formulation, and PEG 400 was used to enhance the drug release. 32 Factorial designs were employed to assess the effect of concentration of HPMCK4M and PEG 400 on the performance of in-situ nasal gel systematically and to optimize the formulation. An optimized in-situ nasal gel was evaluated for appearance, pH, drug content, gelation temperature, mucoadhesive force, viscosity and ex-vivo permeability of drug through nasal mucosa of a goat. Additionally, this formulation was proved to be safe as histopathological studies revealed no deleterious effect on nasal mucosa of a goat after prolonged exposure of 21 days to the optimized formulation. Thus the release of Tramadol Hydrochloride can be sustained if formulated in an in-situ nasal gel containing poloxamer 407 to achieve its prolonged action.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88822789","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00021
Likitha B, F. Sheeba, Yeshavantha Kumar, Shivanand K Mutta, H. S. Keerthy
Emulgel is a fresher class of dosage forms that are prepared by entrapment of large amounts of hydroalcoholic liquid into a network of colloidal solid particles. Emulgel formulations lead to faster drug release compared to ointments and creams. Even supposing gels have many uses but the major difficulty is to delivery of hydrophobic drugs. So, too weak these limitations, emulgels are unit ready. The mixture of gels and emulsions leads to emulgels. Emulsions it's an exact degree of elegance and is of course washed off whenever chosen, they take a high ability to penetrate the skin. Another necessary issue is to increase the drug release of even hydrophilicmedicine by creating w/o emulgel. Among the cluster of solid preparations, the utilization of emulgels has expandedin cosmetics and pharmaceutical preparations. Polymers act as emulsifiers and thickeners as a result of the gelling capability of those compounds permits the formulation of unchanging emulsions and creams by decreasing surface and surface tension and at a similar time increasing the viscosity of the aqueous part. Emulgels area unit is principally used for the delivery of analgesics, medication, anti-fungal, anti-acne medicine, and numerous cosmetic formulations. By applying an appropriate applied mathematics style dissimilar grades of emulgel area unit ready. There area unit numerous favorable properties like being thixotropic, emollient, greaseless, simply spreadable, simply removable, soluble, a longer period, non-staining, bio-friendly, clear and pleasing look. Many penetration enhancers will raise the result.
{"title":"Emulgel: A Novel Topical Drug Delivery","authors":"Likitha B, F. Sheeba, Yeshavantha Kumar, Shivanand K Mutta, H. S. Keerthy","doi":"10.52711/0975-4377.2023.00021","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00021","url":null,"abstract":"Emulgel is a fresher class of dosage forms that are prepared by entrapment of large amounts of hydroalcoholic liquid into a network of colloidal solid particles. Emulgel formulations lead to faster drug release compared to ointments and creams. Even supposing gels have many uses but the major difficulty is to delivery of hydrophobic drugs. So, too weak these limitations, emulgels are unit ready. The mixture of gels and emulsions leads to emulgels. Emulsions it's an exact degree of elegance and is of course washed off whenever chosen, they take a high ability to penetrate the skin. Another necessary issue is to increase the drug release of even hydrophilicmedicine by creating w/o emulgel. Among the cluster of solid preparations, the utilization of emulgels has expandedin cosmetics and pharmaceutical preparations. Polymers act as emulsifiers and thickeners as a result of the gelling capability of those compounds permits the formulation of unchanging emulsions and creams by decreasing surface and surface tension and at a similar time increasing the viscosity of the aqueous part. Emulgels area unit is principally used for the delivery of analgesics, medication, anti-fungal, anti-acne medicine, and numerous cosmetic formulations. By applying an appropriate applied mathematics style dissimilar grades of emulgel area unit ready. There area unit numerous favorable properties like being thixotropic, emollient, greaseless, simply spreadable, simply removable, soluble, a longer period, non-staining, bio-friendly, clear and pleasing look. Many penetration enhancers will raise the result.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78019372","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-05-18DOI: 10.52711/0975-4377.2023.00015
Wajid Ahmad, Jaza Quazi
Chitosan was hydrophobically modified as N-Butyryl chitosan (NBC), N-Lauroyl chitosan (NLC) were synthesized and characterized by FTIR, NMR, XRD, modified chitosan were having about 14 % degree of substitution and varying solubility. Further evaluation of synthesized N-acyl chitosan to loaded Zolmitriptan HCl as nanoparticle by ionotropic method with cross linking by TPP. Average particle size, drug loading, entrapment efficiency and in-vitro mucoadhesion of Zolmitriptan HCl loaded nanoparticle was 150.7±3.3nm, 24.80±1.1% and 54.96±3.8% respectively, with positive zeta potential which were directly correlated with increases bulkiness of the acyl substitution in the modified chitosan except zeta potential was found inversely correlated. TEM and SEM imaging relieved spherical structure of nanoparticle. In vitro release of Zolmitriptan HCl in 1.2 pH HCl buffer and pH 7.4 phosphate buffer solutions showed biphasic release pattern best fitted with Korsmeyer’s-Peppas kinetics with fickian transport mechanism. Acylated chitosan showed sustained release reducing with increasing length of acyl group. Result of the present study showed that hydrophobically modified acylated chitosan can be useful for achieving sustained release controlled by acylation modification.
{"title":"Formulation and Evaluation as Sustain Released Nanoparticles for Zolmitriptan Hydrochloride for the enhanced Bioavailability and Better Therapeutic Action by using Chitosan as a Permeation Enhancer","authors":"Wajid Ahmad, Jaza Quazi","doi":"10.52711/0975-4377.2023.00015","DOIUrl":"https://doi.org/10.52711/0975-4377.2023.00015","url":null,"abstract":"Chitosan was hydrophobically modified as N-Butyryl chitosan (NBC), N-Lauroyl chitosan (NLC) were synthesized and characterized by FTIR, NMR, XRD, modified chitosan were having about 14 % degree of substitution and varying solubility. Further evaluation of synthesized N-acyl chitosan to loaded Zolmitriptan HCl as nanoparticle by ionotropic method with cross linking by TPP. Average particle size, drug loading, entrapment efficiency and in-vitro mucoadhesion of Zolmitriptan HCl loaded nanoparticle was 150.7±3.3nm, 24.80±1.1% and 54.96±3.8% respectively, with positive zeta potential which were directly correlated with increases bulkiness of the acyl substitution in the modified chitosan except zeta potential was found inversely correlated. TEM and SEM imaging relieved spherical structure of nanoparticle. In vitro release of Zolmitriptan HCl in 1.2 pH HCl buffer and pH 7.4 phosphate buffer solutions showed biphasic release pattern best fitted with Korsmeyer’s-Peppas kinetics with fickian transport mechanism. Acylated chitosan showed sustained release reducing with increasing length of acyl group. Result of the present study showed that hydrophobically modified acylated chitosan can be useful for achieving sustained release controlled by acylation modification.","PeriodicalId":20963,"journal":{"name":"Research Journal of Pharmaceutical Dosage Forms and Technology","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74023397","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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