Pub Date : 2018-01-01DOI: 10.2174/1872211312666180213121117
Shruti Sureka, Gaurav Gupta, Mohit Agarwal, Anurag Mishra, Santosh K Singh, Ravindra P Singh, Sushil K Sah, Terezinha de Jesus A Pinto, Kamal Dua
Objective: The current work was attempted to formulate and evaluate the topical sustained release delivery systems called cubosomes containing Tretinoin for the acne treatment. The recent patents on various formulations of tretinoin (EP0408370A2) helped in selecting a new formulation and evaluation.
Methods: Tretinoin loaded cubosomes were prepared by bottom-up technique, using varying the concentration of lipid and surfactant and keeping the drug concentration constant, a total of nine formulations of tretinoin was developed. These preparations were evaluated for surface charge, particle size, particle morphology, encapsulation efficiency, in-vivo and in-vitro release studies of gel enriched with cubosome dispersion. Finally, the stability studies of cubosomal gel were performed on optimized formulations.
Results: Significant result were obtained with tretinoin formulation as the drug is lipophilic, so it gives more depot effect on the epidermis and good retention property. The data obtained from the formulations showed that formulation TCF-5 was the optimized formulation which exhibited better drug release and entrapment efficiency.
Conclusion: It can be concluded that cubosomes offer benefits of quick onset as well as the maximal release of drug with fewer side effects. Thus, cubosomes represent a capable transporter having the property to sustain the release of drug, potential to localize the drug in the skin with a possible clinical application for acne vulgaris treatment due to cubosome depot effect on the epidermis.
{"title":"Formulation, In-Vitro and Ex-Vivo Evaluation of Tretinoin Loaded Cubosomal Gel for the Treatment of Acne.","authors":"Shruti Sureka, Gaurav Gupta, Mohit Agarwal, Anurag Mishra, Santosh K Singh, Ravindra P Singh, Sushil K Sah, Terezinha de Jesus A Pinto, Kamal Dua","doi":"10.2174/1872211312666180213121117","DOIUrl":"https://doi.org/10.2174/1872211312666180213121117","url":null,"abstract":"<p><strong>Objective: </strong>The current work was attempted to formulate and evaluate the topical sustained release delivery systems called cubosomes containing Tretinoin for the acne treatment. The recent patents on various formulations of tretinoin (EP0408370A2) helped in selecting a new formulation and evaluation.</p><p><strong>Methods: </strong>Tretinoin loaded cubosomes were prepared by bottom-up technique, using varying the concentration of lipid and surfactant and keeping the drug concentration constant, a total of nine formulations of tretinoin was developed. These preparations were evaluated for surface charge, particle size, particle morphology, encapsulation efficiency, in-vivo and in-vitro release studies of gel enriched with cubosome dispersion. Finally, the stability studies of cubosomal gel were performed on optimized formulations.</p><p><strong>Results: </strong>Significant result were obtained with tretinoin formulation as the drug is lipophilic, so it gives more depot effect on the epidermis and good retention property. The data obtained from the formulations showed that formulation TCF-5 was the optimized formulation which exhibited better drug release and entrapment efficiency.</p><p><strong>Conclusion: </strong>It can be concluded that cubosomes offer benefits of quick onset as well as the maximal release of drug with fewer side effects. Thus, cubosomes represent a capable transporter having the property to sustain the release of drug, potential to localize the drug in the skin with a possible clinical application for acne vulgaris treatment due to cubosome depot effect on the epidermis.</p>","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"12 2","pages":"121-129"},"PeriodicalIF":0.0,"publicationDate":"2018-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35826770","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}
Hortense Plainfossé, P. Burger, Thomas Michel, Anne Landreau, X. Fernandez
La dermo-cosmetique connait un essor important depuis les annees 1970, les consommateurs etant toujours plus avides de produits aux proprietes averees. Le marche des reparateurs cutanes ne fait pas exception et les allegations revendiquees pour les actifs disponibles sont de plus en plus frequemment certifiees scientifiquement. Apres un rappel concernant le mecanisme de reparation cutanee, differentes methodes permettant de determiner l’activite des ingredients sont presentees dans cet article. Apres une presentation de quelques actifs d’origines synthetique et naturelle, et des eventuels dangers lies a leur utilisation par le consommateur, quelques exemples de formulations cosmetiques sont fournis.
{"title":"Actifs cosmétiques pour la réparation cutanée","authors":"Hortense Plainfossé, P. Burger, Thomas Michel, Anne Landreau, X. Fernandez","doi":"10.51257/a-v1-j3002","DOIUrl":"https://doi.org/10.51257/a-v1-j3002","url":null,"abstract":"La dermo-cosmetique connait un essor important depuis les annees 1970, les consommateurs etant toujours plus avides de produits aux proprietes averees. Le marche des reparateurs cutanes ne fait pas exception et les allegations revendiquees pour les actifs disponibles sont de plus en plus frequemment certifiees scientifiquement. Apres un rappel concernant le mecanisme de reparation cutanee, differentes methodes permettant de determiner l’activite des ingredients sont presentees dans cet article. Apres une presentation de quelques actifs d’origines synthetique et naturelle, et des eventuels dangers lies a leur utilisation par le consommateur, quelques exemples de formulations cosmetiques sont fournis.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83508366","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 : 2017-07-31DOI: 10.2174/1872211311666170117123403
K. Bhupinder, M. Newton
OBJECTIVE The fractionated coconut oil based Solid Lipid Nanoparticles (SLNs) of Acyclovir (ACV) were fabricated in two batches by using Glyceryl mono stearate (GMS) and Lipoid S75 (Fat free soybean phospholipids with 70% phosphatidylcholine-Lipoid GmbH, Germany). The research was focused on developing ACV-SLN by using high pressure hot-homogenization technique. The ingredients were used in different concentrations and ratios to identify the best formulation design. METHODS The GMS with Fractionated coconut oil and Lipoid S75 with Fractionated coconut oil were used in various concentrations in formulation design to assess the impact on the fabrication and evaluation of SLNs. The SLNs were subjected to various characterization techniques such as XRD (X-Ray Diffraction), FTIR (Fourier transform infrared study), master sizer analysis and zeta potential. The mean particle size was determined by master sizer and zeta sizer. Transmission Electron Microscopy (TEM) was used as a tool to analyze the morphology and other features. The zeta potential and drug Entrapment Efficiency (EE%) were also determined. The drug release time profile was studied in vitro study with the utilization of dialysis membrane technique as well as by wistar rat skin. The most recent patents related to the current research topic were also discussed. RESULTS The Zeta potential of the best formulation from GMS batch GNE5 was found to be -2.62mV as the preparation was very viscous with low zeta potential. The better results of Lipoid S75 batch LS4 were found to be 23.23mV which was within the recommended range. The formulations prepared with Lipoid S75, LS4 showed narrow distribution size of 53.46nm and the uniformity was found to be 14.1. The formulation LS4 demonstrated the lowest distribution with of 6.8, 14.5, 139.1nm respectively amongst all the formulations. CONCLUSION SLN dispersions exhibited the average size in nano range. SLNs with small particle size found to have predetermined encapsulation efficiency and relatively high loading capacity and predetermined in vitro drugrelease profile. The lipoid S and Pluronic F68 nanoparticles are found to be superior to Conventional GMSand tween 80 nanoparticles in terms of particles size, stability and zetapotential.
{"title":"Acyclovir Solid Lipid Nanoparticles for Skin Drug Delivery: Fabrication, Characterization and In vitro Study.","authors":"K. Bhupinder, M. Newton","doi":"10.2174/1872211311666170117123403","DOIUrl":"https://doi.org/10.2174/1872211311666170117123403","url":null,"abstract":"OBJECTIVE\u0000The fractionated coconut oil based Solid Lipid Nanoparticles (SLNs) of Acyclovir (ACV) were fabricated in two batches by using Glyceryl mono stearate (GMS) and Lipoid S75 (Fat free soybean phospholipids with 70% phosphatidylcholine-Lipoid GmbH, Germany). The research was focused on developing ACV-SLN by using high pressure hot-homogenization technique. The ingredients were used in different concentrations and ratios to identify the best formulation design.\u0000\u0000\u0000METHODS\u0000The GMS with Fractionated coconut oil and Lipoid S75 with Fractionated coconut oil were used in various concentrations in formulation design to assess the impact on the fabrication and evaluation of SLNs. The SLNs were subjected to various characterization techniques such as XRD (X-Ray Diffraction), FTIR (Fourier transform infrared study), master sizer analysis and zeta potential. The mean particle size was determined by master sizer and zeta sizer. Transmission Electron Microscopy (TEM) was used as a tool to analyze the morphology and other features. The zeta potential and drug Entrapment Efficiency (EE%) were also determined. The drug release time profile was studied in vitro study with the utilization of dialysis membrane technique as well as by wistar rat skin. The most recent patents related to the current research topic were also discussed.\u0000\u0000\u0000RESULTS\u0000The Zeta potential of the best formulation from GMS batch GNE5 was found to be -2.62mV as the preparation was very viscous with low zeta potential. The better results of Lipoid S75 batch LS4 were found to be 23.23mV which was within the recommended range. The formulations prepared with Lipoid S75, LS4 showed narrow distribution size of 53.46nm and the uniformity was found to be 14.1. The formulation LS4 demonstrated the lowest distribution with of 6.8, 14.5, 139.1nm respectively amongst all the formulations.\u0000\u0000\u0000CONCLUSION\u0000SLN dispersions exhibited the average size in nano range. SLNs with small particle size found to have predetermined encapsulation efficiency and relatively high loading capacity and predetermined in vitro drugrelease profile. The lipoid S and Pluronic F68 nanoparticles are found to be superior to Conventional GMSand tween 80 nanoparticles in terms of particles size, stability and zetapotential.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 2 1","pages":"132-146"},"PeriodicalIF":0.0,"publicationDate":"2017-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44062896","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 : 2017-07-31DOI: 10.2174/1872211311666170213105001
K. Krishna, Sidhdhapara T Pradip, S. Navin
BACKGROUND Naratriptan is second-generation triptan class of antimigraine drug which selectively bind with 5-HT(1B/1D) receptor. It is widely used to treat the migraine attack due to its better tolerability and lower recurrence rate as compared to other triptans. Despite of the applicability, Naratriptan also have several drawback like slow onset of action and fist pass metabolism which reduce its efficacy. In order to increase the efficacy of naratriptan fast dissolving film is prepared. METHOD Fast dissolving film of Naratriptan hydrochloride was prepared by solvent casting method Based on the patent survey (US 7648712 B2, WO 2012053006 A2, US 20090047330 A1, EP 2821066 A4, WO 2008108940 A1, WO 2010151020 A3) excipients were screened to find out suitable combination of polymer and plasticizer and Hydroxypropylmethyl Cellulose (HPMC E6) and glycerol were selected as film forming polymer and plasticizer respectively. To study the effect of independent variables on dependent variables 32 full factorial design was applied using Concentration of HPMC E6 and Concentration of Glycerol as independent variables and disintegration time, folding endurance, tensile strength and cumulative % drug release at 2 min as dependent or response variables. A statistical model incorporating interactive and polynomial terms was utilized to evaluate the responses. Result & Conclusion: From the results of statistical evaluation batch F3 was selected as the optimized batch which exhibited shorter disintegration time (22sec) with satisfactory mechanical properties (tensile strength 652.17 gm/mm2). Dissolution of drug from F3 formulation was rapid with around 91% drug release in 120sec. Optimized batch was further evaluated for in vitro permeation study using Franz diffusion cell.
{"title":"Preparation and Optimization of Fast Dissolving Film of Naratr iptan Hydrochloride.","authors":"K. Krishna, Sidhdhapara T Pradip, S. Navin","doi":"10.2174/1872211311666170213105001","DOIUrl":"https://doi.org/10.2174/1872211311666170213105001","url":null,"abstract":"BACKGROUND\u0000Naratriptan is second-generation triptan class of antimigraine drug which selectively bind with 5-HT(1B/1D) receptor. It is widely used to treat the migraine attack due to its better tolerability and lower recurrence rate as compared to other triptans. Despite of the applicability, Naratriptan also have several drawback like slow onset of action and fist pass metabolism which reduce its efficacy. In order to increase the efficacy of naratriptan fast dissolving film is prepared.\u0000\u0000\u0000METHOD\u0000Fast dissolving film of Naratriptan hydrochloride was prepared by solvent casting method Based on the patent survey (US 7648712 B2, WO 2012053006 A2, US 20090047330 A1, EP 2821066 A4, WO 2008108940 A1, WO 2010151020 A3) excipients were screened to find out suitable combination of polymer and plasticizer and Hydroxypropylmethyl Cellulose (HPMC E6) and glycerol were selected as film forming polymer and plasticizer respectively. To study the effect of independent variables on dependent variables 32 full factorial design was applied using Concentration of HPMC E6 and Concentration of Glycerol as independent variables and disintegration time, folding endurance, tensile strength and cumulative % drug release at 2 min as dependent or response variables. A statistical model incorporating interactive and polynomial terms was utilized to evaluate the responses. Result & Conclusion: From the results of statistical evaluation batch F3 was selected as the optimized batch which exhibited shorter disintegration time (22sec) with satisfactory mechanical properties (tensile strength 652.17 gm/mm2). Dissolution of drug from F3 formulation was rapid with around 91% drug release in 120sec. Optimized batch was further evaluated for in vitro permeation study using Franz diffusion cell.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 2 1","pages":"124-131"},"PeriodicalIF":0.0,"publicationDate":"2017-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46509389","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 : 2017-07-31DOI: 10.2174/187221131102171220154222
Brahma N. Singh
{"title":"Meet Our Associate Editor","authors":"Brahma N. Singh","doi":"10.2174/187221131102171220154222","DOIUrl":"https://doi.org/10.2174/187221131102171220154222","url":null,"abstract":"","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 1","pages":"81-81"},"PeriodicalIF":0.0,"publicationDate":"2017-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/187221131102171220154222","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48459058","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 : 2017-07-06DOI: 10.2174/1872211311666170118112002
Sarode D Harshada, A. Mundada
BACKGROUND Nasal inserts are novel, solid, bioadhesive dosage forms administered via nasal route for prolonged systemic drug delivery. The principle of the dosage form is that, after administration nasal inserts imbibe nasal fluid from the mucosa and form a gel in the nasal cavity in order to avoid foreign body sensation. The objective of this investigation was the development of chitosan/xanthan gum based bioadhesive nasal inserts of antimigraine drug. METHODS Lyophilization is more usual technique for the preparation of nasal inserts and it is one of the applied methods for drying of solids either in the form of aqueous solution or rarely in the form of aqueous suspension by using freeze dryers. The recent patents on Biocompatible polymer (US20140301972A1), High molecular weight polymers (US20050048121A1), Migraine treatment (WO2009080764A3) helped in selecting the drug and polymers. A 32 factorial design was used to investigate the combined effect of two independent variables such as concentration of Xanthan gum (X1) and the concentration of Chitosan (X2), onto the water uptake, bioadhesion potential and drug release which were the dependent variables. Nine batches of the nasal inserts were developed and evaluated for water uptake at three different pH, bioadhesion potential and drug release. The optimized nasal inserts batch was also characterized by DSC, PXRD and SEM. RESULTS The results showed that the water uptake ability of nasal insert was strongly influenced by pH of the medium and by polycation/polyanion concentration. This investigation verifies the formation of complexes between chitosan and xanthan gum and confirms the potential of these complexes, in achieving the sustained antimigraine drug delivery in the nasal cavity. CONCLUSION The best nasal inserts formulation containing chitosan and xanthan gum in the ratio 0.5:0.5, showed desirable % drug release as well as bioadhesion which may result in an increase in the nasal residence time.
{"title":"Formulation Development and Evaluation of Lyophilized Nasal Inserts for Migraine Treatment.","authors":"Sarode D Harshada, A. Mundada","doi":"10.2174/1872211311666170118112002","DOIUrl":"https://doi.org/10.2174/1872211311666170118112002","url":null,"abstract":"BACKGROUND\u0000Nasal inserts are novel, solid, bioadhesive dosage forms administered via nasal route for prolonged systemic drug delivery. The principle of the dosage form is that, after administration nasal inserts imbibe nasal fluid from the mucosa and form a gel in the nasal cavity in order to avoid foreign body sensation. The objective of this investigation was the development of chitosan/xanthan gum based bioadhesive nasal inserts of antimigraine drug.\u0000\u0000\u0000METHODS\u0000Lyophilization is more usual technique for the preparation of nasal inserts and it is one of the applied methods for drying of solids either in the form of aqueous solution or rarely in the form of aqueous suspension by using freeze dryers. The recent patents on Biocompatible polymer (US20140301972A1), High molecular weight polymers (US20050048121A1), Migraine treatment (WO2009080764A3) helped in selecting the drug and polymers. A 32 factorial design was used to investigate the combined effect of two independent variables such as concentration of Xanthan gum (X1) and the concentration of Chitosan (X2), onto the water uptake, bioadhesion potential and drug release which were the dependent variables. Nine batches of the nasal inserts were developed and evaluated for water uptake at three different pH, bioadhesion potential and drug release. The optimized nasal inserts batch was also characterized by DSC, PXRD and SEM.\u0000\u0000\u0000RESULTS\u0000The results showed that the water uptake ability of nasal insert was strongly influenced by pH of the medium and by polycation/polyanion concentration. This investigation verifies the formation of complexes between chitosan and xanthan gum and confirms the potential of these complexes, in achieving the sustained antimigraine drug delivery in the nasal cavity.\u0000\u0000\u0000CONCLUSION\u0000The best nasal inserts formulation containing chitosan and xanthan gum in the ratio 0.5:0.5, showed desirable % drug release as well as bioadhesion which may result in an increase in the nasal residence time.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 1 1","pages":"42-53"},"PeriodicalIF":0.0,"publicationDate":"2017-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49169117","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 : 2017-03-31DOI: 10.2174/1872211311666170105114459
S. Patwardhan, M. Patil, Anbazhagan Sockalingam
BACKGROUND The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients. METHOD Current protocol employs various extracts of Piper cubeba fruit to evaluate its role in absorption of NPRS. Various batches containing 1% NPRS and varying concentrations of synthetic permeation enhancers or the extracts were formulated in carbopol gel. Gel was evaluated for parameters like organoleptic parameters, pH, viscosity and spreadability. An ex-vivo percutaneous absorption of NPRS from gel was investigated and compared with best performing synthetic enhancer, transcutol P (TP). RESULT The batch containing 2% n-hexane extract (NHE) of Piper cubeba showed higher permeation than TP and Chloroform (CE), Methanolic (ME) and aqueous (AE) extracts as well. It showed improved % cumulative release (85.09%) and flux (278.61μg/cm2.h), as compared to TP and other extracts. Histopathology indicated the formulation safer as compared to that with synthetic enhancer. CONCLUSION It suggests P. cubeba as effective and safer tool for transdermal delivery and acts as therapeutic facilitator for naproxen. GC-MS analysis indicates lignans & terpenes in NHE to which this permeation enhancement activity may be attributed.
背景:药物经皮肤吸收，避免了口服方式的许多副作用，如胃刺激、恶心、全身毒性等，从而提高了患者的依从性。萘普生钠(NPRS)是一种有效的非甾体抗炎药。目的研制和评价含有NPRS的经皮给药凝胶制剂，减少副作用，提高患者依从性。非甾体抗炎药局部给药专利(US 9012402 B1, US 9072659 B2, US 20150258196 A1)和草药渗透增强剂专利(US 20100273746A1, WO 2005009510 A2, US 6004969 A)有助于选择药物和辅料。方法采用不同提取方法，评价其对NPRS的吸收作用。在卡波波尔凝胶中配制了含有1% NPRS和不同浓度的合成渗透增强剂或提取物的不同批次。评价凝胶的感官参数、pH、粘度和涂抹性等参数。研究了凝胶中NPRS的体外经皮吸收，并与性能最好的合成增强剂transcutol P (TP)进行了比较。结果2%正己烷提取物(NHE)比TP、氯仿(CE)、甲醇(ME)和水提液(AE)具有更高的渗透性。与TP和其他提取物相比，其%累积释放量(85.09%)和通量(278.61μg/cm2.h)均有所提高。组织病理学结果表明，该制剂较合成增强剂更安全。结论丁香是一种安全有效的经皮给药工具，可作为萘普生的促药剂。GC-MS分析表明，这种渗透增强活性可能归因于NHE中的木脂素和萜烯。
{"title":"Development and Evaluation of Naproxen Sodium Gel Using Piper cubeba for Enhanced Transdermal Drug Delivery and Therapeutic Facilitation.","authors":"S. Patwardhan, M. Patil, Anbazhagan Sockalingam","doi":"10.2174/1872211311666170105114459","DOIUrl":"https://doi.org/10.2174/1872211311666170105114459","url":null,"abstract":"BACKGROUND\u0000The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents.\u0000\u0000\u0000OBJECTIVE\u0000The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients.\u0000\u0000\u0000METHOD\u0000Current protocol employs various extracts of Piper cubeba fruit to evaluate its role in absorption of NPRS. Various batches containing 1% NPRS and varying concentrations of synthetic permeation enhancers or the extracts were formulated in carbopol gel. Gel was evaluated for parameters like organoleptic parameters, pH, viscosity and spreadability. An ex-vivo percutaneous absorption of NPRS from gel was investigated and compared with best performing synthetic enhancer, transcutol P (TP).\u0000\u0000\u0000RESULT\u0000The batch containing 2% n-hexane extract (NHE) of Piper cubeba showed higher permeation than TP and Chloroform (CE), Methanolic (ME) and aqueous (AE) extracts as well. It showed improved % cumulative release (85.09%) and flux (278.61μg/cm2.h), as compared to TP and other extracts. Histopathology indicated the formulation safer as compared to that with synthetic enhancer.\u0000\u0000\u0000CONCLUSION\u0000It suggests P. cubeba as effective and safer tool for transdermal delivery and acts as therapeutic facilitator for naproxen. GC-MS analysis indicates lignans & terpenes in NHE to which this permeation enhancement activity may be attributed.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 1 1","pages":"28-35"},"PeriodicalIF":0.0,"publicationDate":"2017-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48282030","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 : 2017-03-31DOI: 10.2174/1872211310666161216111515
Ashwathanarayana Madhu, G. Gupta, Bharati Arali, D. Chellappan, K. Dua
AIMS AND BACKGROUND Psychosis is a neurological disorder, which is usually defined as the "loss of contact with reality." As medicine 'Hemidesmusindicus' holds a reputed place in all systems of medicine in India. It is given in the form of infusion, fine particles, or syrup. It is also a component of several medicinal preparations. The present research work is pertaining to find out an anti-psychotic activity of an aqueous root extract of Hemidesmusindicus- a time bound study in rats. METHODS In the present study, the dried roots of Hemidesmusindicus were crushed to a coarse powder and extracted with water under reflux for 36 hours to obtain the aqueous extract of roots of Hemidesmusindicus (AERHI). The extract was reconstituted in 2% aqueous tragacanth just before use and administered orally at a dose 0f 100 mg/kg, 300 mg/kg and 500 mg/kg. In a single dose study, the parameters were assessed after oral administration of the single dose of the AERHI, whereas in a multiple dose study, the animals daily received the suitable oral dose of the AERHI for a period of 30 days. The parameters were assessed on the 15th and 30th day. The antipsychotic activity was screened using Apomorphine induced Stereotyped behavior in rats and Haloperidol induced catalepsy models were used. In Apomorphine induced Stereotyped behavior inhibition of the Stereotyped behavior was considered to be anti-psychotic activity and in Haloperidol induced catalepsy, we observed whether the AERHI potentate or attenuate the catalepsy in rats. RESULTS In this study, the extract of Hemidesmusindicus significantly inhibited the stereotyped behavior induced by apomorphine in rats and also potentiate the catalepsy induced by haloperidol, thereby showing its anti-psychotic activity. CONCLUSION All these observations imply that Hemidesmusindicus extract possesses anti-psychotic activity in experimental animals.
{"title":"Anti-Psychotic Activity of Aqueous Root Extract of Hemidesmus indicus: A Time Bound Study in Rats.","authors":"Ashwathanarayana Madhu, G. Gupta, Bharati Arali, D. Chellappan, K. Dua","doi":"10.2174/1872211310666161216111515","DOIUrl":"https://doi.org/10.2174/1872211310666161216111515","url":null,"abstract":"AIMS AND BACKGROUND\u0000Psychosis is a neurological disorder, which is usually defined as the \"loss of contact with reality.\" As medicine 'Hemidesmusindicus' holds a reputed place in all systems of medicine in India. It is given in the form of infusion, fine particles, or syrup. It is also a component of several medicinal preparations. The present research work is pertaining to find out an anti-psychotic activity of an aqueous root extract of Hemidesmusindicus- a time bound study in rats.\u0000\u0000\u0000METHODS\u0000In the present study, the dried roots of Hemidesmusindicus were crushed to a coarse powder and extracted with water under reflux for 36 hours to obtain the aqueous extract of roots of Hemidesmusindicus (AERHI). The extract was reconstituted in 2% aqueous tragacanth just before use and administered orally at a dose 0f 100 mg/kg, 300 mg/kg and 500 mg/kg. In a single dose study, the parameters were assessed after oral administration of the single dose of the AERHI, whereas in a multiple dose study, the animals daily received the suitable oral dose of the AERHI for a period of 30 days. The parameters were assessed on the 15th and 30th day. The antipsychotic activity was screened using Apomorphine induced Stereotyped behavior in rats and Haloperidol induced catalepsy models were used. In Apomorphine induced Stereotyped behavior inhibition of the Stereotyped behavior was considered to be anti-psychotic activity and in Haloperidol induced catalepsy, we observed whether the AERHI potentate or attenuate the catalepsy in rats.\u0000\u0000\u0000RESULTS\u0000In this study, the extract of Hemidesmusindicus significantly inhibited the stereotyped behavior induced by apomorphine in rats and also potentiate the catalepsy induced by haloperidol, thereby showing its anti-psychotic activity.\u0000\u0000\u0000CONCLUSION\u0000All these observations imply that Hemidesmusindicus extract possesses anti-psychotic activity in experimental animals.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 1 1","pages":"36-41"},"PeriodicalIF":0.0,"publicationDate":"2017-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41878372","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 : 2017-03-31DOI: 10.2174/1872211311666170213104321
R. Taneja, G. Gupta
BACKGROUND To develop pulsatile microspheres of Nifedipine blend of polymers Carbopol 971P and Eudragit RS100 for antihypertensive to release the drug at a particular lag time. METHODS Pulsatile nifedipine microspheres were prepared using the blend of Carbopol 971P and Eudragit RS100 at different ratios in a mixture of solvents. Formulations were prepared and optimized on the basis of particle size, percentage yield and drug entrapment efficiency. Optimized formulations were further analyzed at different resolutions per minute (rpm) by optical microscopy, scanning electron microscopy (SEM), in-vitro dissolution studies and kinetics model. The most promising formulation was compared with the marketed products. The recent patents on microsphere used for hypertension for drug used Liensinine (CN104757561). Dopamine antagonist (US20030069232A1), Human Serum Albumin (EP19990304616) and Omeprazole (IN2107/DEL/2014) helped in selecting the drug and polymers. RESULTS The formulated microspheres had mean particle size ranging from 177.31 to 277.48 µm. Formulation F83 showed slow release of drug initially for 4 h and drastically release of drug enhanced at a particular lag time (Showed pulsatile release) after 6 h. However, conventional marketed products showed maximum release initially at 1 h and decreased gradually while controlled released marketed product showed sustained pattern. CONCLUSION On the basis of data formulation F83 showed slow release and at a particular lag time followed by pulsatile release pattern and followed first order kinetics model. It was concluded that the formulated nifedipine pulsatile dosage form could be useful in the treatment of hypertension.
{"title":"Development and Characterization Pulsatile Microspheres of Nifedipine for Hypertension.","authors":"R. Taneja, G. Gupta","doi":"10.2174/1872211311666170213104321","DOIUrl":"https://doi.org/10.2174/1872211311666170213104321","url":null,"abstract":"BACKGROUND\u0000To develop pulsatile microspheres of Nifedipine blend of polymers Carbopol 971P and Eudragit RS100 for antihypertensive to release the drug at a particular lag time.\u0000\u0000\u0000METHODS\u0000Pulsatile nifedipine microspheres were prepared using the blend of Carbopol 971P and Eudragit RS100 at different ratios in a mixture of solvents. Formulations were prepared and optimized on the basis of particle size, percentage yield and drug entrapment efficiency. Optimized formulations were further analyzed at different resolutions per minute (rpm) by optical microscopy, scanning electron microscopy (SEM), in-vitro dissolution studies and kinetics model. The most promising formulation was compared with the marketed products. The recent patents on microsphere used for hypertension for drug used Liensinine (CN104757561). Dopamine antagonist (US20030069232A1), Human Serum Albumin (EP19990304616) and Omeprazole (IN2107/DEL/2014) helped in selecting the drug and polymers.\u0000\u0000\u0000RESULTS\u0000The formulated microspheres had mean particle size ranging from 177.31 to 277.48 µm. Formulation F83 showed slow release of drug initially for 4 h and drastically release of drug enhanced at a particular lag time (Showed pulsatile release) after 6 h. However, conventional marketed products showed maximum release initially at 1 h and decreased gradually while controlled released marketed product showed sustained pattern.\u0000\u0000\u0000CONCLUSION\u0000On the basis of data formulation F83 showed slow release and at a particular lag time followed by pulsatile release pattern and followed first order kinetics model. It was concluded that the formulated nifedipine pulsatile dosage form could be useful in the treatment of hypertension.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 1 1","pages":"67-76"},"PeriodicalIF":0.0,"publicationDate":"2017-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47875799","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 : 2017-03-31DOI: 10.2174/1872211310666161004160304
P. Deb, J. Singha, Indranil Chanda, P. Chakraborty
BACKGROUND The aim of the present investigation is to formulate and optimize oral sustained release matrix tablet of highly water soluble drug Tramadol HCl and to evaluate the effect of varying concentration of hydrophilic and hydrophobic polymer on drug release, based on a survey done on the recent patents of Tramadol HCl (US7374781, CA 2479252) and sustained release matrix tablets. METHODS The tablets were prepared by double granulation process, by melt granulation and wet granulation technique using Carnauba wax (CW) and HPMC K100 as release retardant. RESULTS Pre and post compression factors were evaluated and all the parameters were found within the limit. The drug release data were subjected to different models in order to evaluate release kinetics and mechanism of drug release. The prepared formulations showed drug release in the range 100±2% in 6hrs, 7hrs, 8hrs and 9hrs and upto 12 hrs respectively. The optimized tablet having 25% CW and 20% HPMC showed sustained drug release pattern. Hydrophilic matrix of HPMC alone could not control the Tramadol release effectively for 12 h whereas when combined with CW could slow down the release of drug and can be successfully employed for formulating sustained-release matrix tablets. Similarity factor, f2 shows the test and reference profile are identical. CONCLUSION Double granulation technique with CW and HPMC K100 proved as a better technique for sustaining the drug release from the matrix tablet.
{"title":"Formulation Development and Optimization of Matrix Tablet of Tramadol Hydrochloride.","authors":"P. Deb, J. Singha, Indranil Chanda, P. Chakraborty","doi":"10.2174/1872211310666161004160304","DOIUrl":"https://doi.org/10.2174/1872211310666161004160304","url":null,"abstract":"BACKGROUND\u0000The aim of the present investigation is to formulate and optimize oral sustained release matrix tablet of highly water soluble drug Tramadol HCl and to evaluate the effect of varying concentration of hydrophilic and hydrophobic polymer on drug release, based on a survey done on the recent patents of Tramadol HCl (US7374781, CA 2479252) and sustained release matrix tablets.\u0000\u0000\u0000METHODS\u0000The tablets were prepared by double granulation process, by melt granulation and wet granulation technique using Carnauba wax (CW) and HPMC K100 as release retardant.\u0000\u0000\u0000RESULTS\u0000Pre and post compression factors were evaluated and all the parameters were found within the limit. The drug release data were subjected to different models in order to evaluate release kinetics and mechanism of drug release. The prepared formulations showed drug release in the range 100±2% in 6hrs, 7hrs, 8hrs and 9hrs and upto 12 hrs respectively. The optimized tablet having 25% CW and 20% HPMC showed sustained drug release pattern. Hydrophilic matrix of HPMC alone could not control the Tramadol release effectively for 12 h whereas when combined with CW could slow down the release of drug and can be successfully employed for formulating sustained-release matrix tablets. Similarity factor, f2 shows the test and reference profile are identical.\u0000\u0000\u0000CONCLUSION\u0000Double granulation technique with CW and HPMC K100 proved as a better technique for sustaining the drug release from the matrix tablet.","PeriodicalId":40024,"journal":{"name":"Recent Patents on Drug Delivery and Formulation","volume":"11 1 1","pages":"19-27"},"PeriodicalIF":0.0,"publicationDate":"2017-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43466431","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}
扫码关注我们
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号