Pub Date : 2019-03-31DOI: 10.37285/ijpsn.2019.12.2.3
Laxmi Raj A, Y. Kumar
The study was aimed to formulate solid dispersions of Manidipine by using different novel carriers like Labrafac PG, Kolliwax RH 40, Soluplus, Kolliwax GMS II, Kolliphor EL and SLS in drug carrier ratio by using solvent evaporation method. The formulations were characterized for physical appearance, solubility and in vitro dissolution studies. The optimized formulation was characterized and Formulation SD13 was found to be optimized one based on the solubility, dissolution and other parameters using Kolliwax GMS II and SLS. The drug release of the optimized formulation was found to be 99.41±5.38% within 90 min. Powder X-ray diffraction studies performed on solid dispersion showed that Manidipine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Manidipine to an amorphous form. Therefore, the solid dispersions using Kolliwax GMS II as hydrophilic carrier in the combination of SLS can be successfully used for improvement of solubility and dissolution of Manidipine.
{"title":"Formulation, Characterization and Solubility Enhancement of Manidipine Solid Dispersions","authors":"Laxmi Raj A, Y. Kumar","doi":"10.37285/ijpsn.2019.12.2.3","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.2.3","url":null,"abstract":"The study was aimed to formulate solid dispersions of Manidipine by using different novel carriers like Labrafac PG, Kolliwax RH 40, Soluplus, Kolliwax GMS II, Kolliphor EL and SLS in drug carrier ratio by using solvent evaporation method. The formulations were characterized for physical appearance, solubility and in vitro dissolution studies. The optimized formulation was characterized and Formulation SD13 was found to be optimized one based on the solubility, dissolution and other parameters using Kolliwax GMS II and SLS. The drug release of the optimized formulation was found to be 99.41±5.38% within 90 min. Powder X-ray diffraction studies performed on solid dispersion showed that Manidipine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Manidipine to an amorphous form. Therefore, the solid dispersions using Kolliwax GMS II as hydrophilic carrier in the combination of SLS can be successfully used for improvement of solubility and dissolution of Manidipine. ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"7 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79601923","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 : 2019-03-31DOI: 10.37285/ijpsn.2019.12.2.4
K TarakaSunilKumar, M. Varma, P RaviPrakash
Solid-lipid nanoparticles (SLNs) are an alternative carrier system used for loading the drug for targeting, improving the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nanometric size range so that the liver cannot uptake the drug from the delivery system and is not metabolized by the liver. Bortezomib is an anti-cancer drug. Due to its poor oral bioavailability, presystemic metabolism and decreased half-life, it was chosen to formulate as the SLN system with the use of a 3-factor, 3-level Box–Behnken design, by hot homogenization followed by an ultrasonication method. Trimyristin (Dynasan-114), tripalmitin (Dynasan 116) and tristearin (Dynasan-118) were used as lipids and based on the results from the initial studies tripalmitin (Dynasan116) was selected as the lipid for the further studies along with phosphatidylcholine as surfactant and Poloxamer 188 as stabilizer. The optimized formulation (F1) was obtained with minimum particle size (204 nm), maximum entrapment efficiency (70.24) and drug loading (21.24). The optimised batches were further investigated by FTIR, DSC, XRD, SEM and stability. In vitro release studies showed that maximum cumulative drug release was obtained for F1 (99.74%). The optimized formulation Bortezomib followed zero-order release kinetics with a strong correlation coefficient (R2= 0.9994). The nanoformulation prepared under optimized conditions is in concurrence with the expected results. It is concluded that the SLN formulation can be used as a potential carrier for the effective delivery of Bortezomib.
{"title":"Formulation and Optimization of Solid-Lipid Nano-particles of the Anticancer Drug Bortezomib","authors":"K TarakaSunilKumar, M. Varma, P RaviPrakash","doi":"10.37285/ijpsn.2019.12.2.4","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.2.4","url":null,"abstract":"Solid-lipid nanoparticles (SLNs) are an alternative carrier system used for loading the drug for targeting, improving the bioavailability by increasing its solubility, and protecting the drug from presystemic metabolism. The avoidance of presystemic metabolism is due to the nanometric size range so that the liver cannot uptake the drug from the delivery system and is not metabolized by the liver. Bortezomib is an anti-cancer drug. Due to its poor oral bioavailability, presystemic metabolism and decreased half-life, it was chosen to formulate as the SLN system with the use of a 3-factor, 3-level Box–Behnken design, by hot homogenization followed by an ultrasonication method. Trimyristin (Dynasan-114), tripalmitin (Dynasan 116) and tristearin (Dynasan-118) were used as lipids and based on the results from the initial studies tripalmitin (Dynasan116) was selected as the lipid for the further studies along with phosphatidylcholine as surfactant and Poloxamer 188 as stabilizer. The optimized formulation (F1) was obtained with minimum particle size (204 nm), maximum entrapment efficiency (70.24) and drug loading (21.24). The optimised batches were further investigated by FTIR, DSC, XRD, SEM and stability. In vitro release studies showed that maximum cumulative drug release was obtained for F1 (99.74%). The optimized formulation Bortezomib followed zero-order release kinetics with a strong correlation coefficient (R2= 0.9994). The nanoformulation prepared under optimized conditions is in concurrence with the expected results. It is concluded that the SLN formulation can be used as a potential carrier for the effective delivery of Bortezomib.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"99 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78381171","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 : 2019-03-31DOI: 10.37285/ijpsn.2019.12.2.6
R. Kaza, S. M, K. M, A. A., Nagaraju R
This research work was aimed to develop the telmisartan fast dissolving films. Fast dissolving films allow rapid drug dissolution in the oral cavity and thereby bypass the first pass metabolism. Solid dispersions of telmisartan using natural polymers such as hupu gum (HG), guar gum (GG) and xanthan gum (XG) were prepared by kneading technique and the optimized solid dispersion was exploited in the development of rapidly dissolving film. Telmisartan films were prepared by solvent casting method using different grades of HPMC (E5, 50 cps and K4M). Six formulations (FT1-FT6) of telmisartan films were prepared and evaluated for their physical characteristics such as thickness, tensile strength, percentage elongation, weight variation, folding endurance, drug content uniformity and surface pH and gave satisfactory results. The compatibility of the drug in the formulation was confirmed by FTIR and DSC studies. The formulations were subjected to disintegration, in vitro drug release and pharmacodynamic studies on spontaneous hypertensive rats (SHR). Amongst the formulations of FT1-FT6, FT6 was found as best formulation which contains HPMC E5 and telmisartan solid dispersion with guar gum at weight ratio of 1:2 and showed excellent film forming characteristics such as disintegration time at 42 sec and percentage drug release 97.98% within 10 minutes. The optimized film formulation (FT6) showed excellent stability over 45 days when stored at 40°C/60% RH. The pharmacodynamic study in SHR proved that fast dissolving films of telmisartan produced a faster onset of action.
{"title":"Biopharmaceutical and Pharmacodynamic Characteri-stics of Telmisartan Oral Disintegrating Films","authors":"R. Kaza, S. M, K. M, A. A., Nagaraju R","doi":"10.37285/ijpsn.2019.12.2.6","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.2.6","url":null,"abstract":"\u0000This research work was aimed to develop the telmisartan fast dissolving films. Fast dissolving films allow rapid drug dissolution in the oral cavity and thereby bypass the first pass metabolism. Solid dispersions of telmisartan using natural polymers such as hupu gum (HG), guar gum (GG) and xanthan gum (XG) were prepared by kneading technique and the optimized solid dispersion was exploited in the development of rapidly dissolving film. Telmisartan films were prepared by solvent casting method using different grades of HPMC (E5, 50 cps and K4M). Six formulations (FT1-FT6) of telmisartan films were prepared and evaluated for their physical characteristics such as thickness, tensile strength, percentage elongation, weight variation, folding endurance, drug content uniformity and surface pH and gave satisfactory results. The compatibility of the drug in the formulation was confirmed by FTIR and DSC studies. The formulations were subjected to disintegration, in vitro drug release and pharmacodynamic studies on spontaneous hypertensive rats (SHR). Amongst the formulations of FT1-FT6, FT6 was found as best formulation which contains HPMC E5 and telmisartan solid dispersion with guar gum at weight ratio of 1:2 and showed excellent film forming characteristics such as disintegration time at 42 sec and percentage drug release 97.98% within 10 minutes. The optimized film formulation (FT6) showed excellent stability over 45 days when stored at 40°C/60% RH. The pharmacodynamic study in SHR proved that fast dissolving films of telmisartan produced a faster onset of action. \u0000 ","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82272468","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 : 2019-01-31DOI: 10.37285/ijpsn.2019.12.1.7
Bhikshapathi D.v.r.n., B RamPrasad
{"title":"Formulation Development and In vitro Evaluation of Controlled Release Gliclazide Trilayer Matrix Tablets by Geomatrix Technology","authors":"Bhikshapathi D.v.r.n., B RamPrasad","doi":"10.37285/ijpsn.2019.12.1.7","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.1.7","url":null,"abstract":"","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"18 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88337241","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 : 2019-01-31DOI: 10.37285/ijpsn.2019.12.1.4
Padmini Thatavarthi, Rajkamal Bigala
{"title":"One-pot Synthesis and Antimicrobial Activities of N-Substituted Pyrazoles from Nitro-olefins and Hydrazones","authors":"Padmini Thatavarthi, Rajkamal Bigala","doi":"10.37285/ijpsn.2019.12.1.4","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.1.4","url":null,"abstract":"","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"59 2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83729675","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 : 2019-01-31DOI: 10.37285/ijpsn.2019.12.1.6
R. K. Kota, D V R N Bhikshapath, S. Gande
{"title":"Formulation and In vivo Evaluation of Mucoadhesive Microspheres of Valsartan using Natural Gum","authors":"R. K. Kota, D V R N Bhikshapath, S. Gande","doi":"10.37285/ijpsn.2019.12.1.6","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.1.6","url":null,"abstract":"","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"41 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81515780","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 : 2019-01-31DOI: 10.37285/ijpsn.2019.12.1.8
Ashok Kumar Uppuluru, S. Gande
{"title":"Enhancement of Solubility and Dissolution Rate of Lercanidipine Solid Dispersions","authors":"Ashok Kumar Uppuluru, S. Gande","doi":"10.37285/ijpsn.2019.12.1.8","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.1.8","url":null,"abstract":"","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"76 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76002784","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 : 2019-01-31DOI: 10.37285/ijpsn.2019.12.1.5
C. Suja, E. K Jinisha
{"title":"Formulation and Evaluation of Fast Dissolving Meben-dazole Tablets using Different Superdisintegrants","authors":"C. Suja, E. K Jinisha","doi":"10.37285/ijpsn.2019.12.1.5","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.1.5","url":null,"abstract":"","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"40 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75070382","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 : 2019-01-31DOI: 10.37285/ijpsn.2019.12.1.2
Abhishek Kumar, Amit Pandey.K, M. Koshy
Targeting drugs directly to the colon is advantageous in the topical treatment of colonic diseases such as ulcerative colitis and Crohn’s disease and has shown potential in gaining the oral delivery of peptides and other labile drugs. A colonic drug delivery system is required to protect a drug during its transit through the upper gastro-intestinal (G.I.T.) tract and allow its release in the colon. Several methods of colonic targeting have been proposed. These include taking advantage of the apparent consistency of small intestinal transit times, the utilization of pH changes within the G.I. tract and the exploitation of bacterial enzymes localized in the colonic region of the G.I. tract. Among the different approaches to achieve targeted drug release to the colon, the use of polymers especially biodegradable by colonic bacteria holds great promise. Polysaccharides are bacterial enzymes that are available in sufficient quantity to be exploited in colon targeting of drugs. Based on this approach, various polysaccharides have been investigated for colon-specific drug release. These polysaccharides include pectin, guar gum, amylose, inulin, dextran, chitosan, and chondroitin sulfate. This family of natural polymers has an appeal to drug delivery as it is comprised of polymers with a large number of derivatizable groups, a wide range of molecular weights, varying chemical compositions, and, for the most part, low toxicity and biodegradability yet high stability. The most favorable property of these materials is their approval as pharmaceutical excipients. Polysaccharides are bacterial enzymes that are available in sufficient quantity to degrade these natural polysaccharides.
{"title":"Characteristics of Natural Polysaccharides for Colon Drug Targeting","authors":"Abhishek Kumar, Amit Pandey.K, M. Koshy","doi":"10.37285/ijpsn.2019.12.1.2","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.1.2","url":null,"abstract":"Targeting drugs directly to the colon is advantageous in the topical treatment of colonic diseases such as ulcerative colitis and Crohn’s disease and has shown potential in gaining the oral delivery of peptides and other labile drugs. A colonic drug delivery system is required to protect a drug during its transit through the upper gastro-intestinal (G.I.T.) tract and allow its release in the colon. Several methods of colonic targeting have been proposed. These include taking advantage of the apparent consistency of small intestinal transit times, the utilization of pH changes within the G.I. tract and the exploitation of bacterial enzymes localized in the colonic region of the G.I. tract. Among the different approaches to achieve targeted drug release to the colon, the use of polymers especially biodegradable by colonic bacteria holds great promise. Polysaccharides are bacterial enzymes that are available in sufficient quantity to be exploited in colon targeting of drugs. Based on this approach, various polysaccharides have been investigated for colon-specific drug release. These polysaccharides include pectin, guar gum, amylose, inulin, dextran, chitosan, and chondroitin sulfate. This family of natural polymers has an appeal to drug delivery as it is comprised of polymers with a large number of derivatizable groups, a wide range of molecular weights, varying chemical compositions, and, for the most part, low toxicity and biodegradability yet high stability. The most favorable property of these materials is their approval as pharmaceutical excipients. Polysaccharides are bacterial enzymes that are available in sufficient quantity to degrade these natural polysaccharides.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"48 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88684060","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 : 2019-01-31DOI: 10.37285/ijpsn.2019.12.1.3
Reena Ughreja, R. Parikh
{"title":"Optimization of Ethyl Cellulose Microspheres Containing Satranidazole Using 32 Factorial Design","authors":"Reena Ughreja, R. Parikh","doi":"10.37285/ijpsn.2019.12.1.3","DOIUrl":"https://doi.org/10.37285/ijpsn.2019.12.1.3","url":null,"abstract":"","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"43 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88056840","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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