Pub Date : 2022-03-30DOI: 10.2174/2210303112666220330124251
M. Dholakia, Dinal Patel, Harshida Chauhan, B. Suhagia
The present study developed oral in-situ gel containing the leaf extract of Taraxacum officinale (T.O.) using the Design of the experiment. Background: Peptic ulcer disease is an epidemic in the 19th and early 20th centuries. The application of herbal drugs for peptic diseases is an attractive area for research and implementation as compared to the allopathic system in the recent era. From the number of plants, the antioxidant effect of an aqueous extract of Taraxacum officinale that is Dandelion leaf was proven by an animal study in some previous literature. However, most of the marketed preparations consist root extract primarily used for detoxification of liver incomparision to the leaf extract having nonspecific application. Hence the aqueous extract of Dandelion leaf was taken as the active ingredient in the formulation. Over the past 30 years, greater attention has been focused on the development of controlled and sustained drug delivery systems. The development of in situ gel systems has received considerable attention over the past few years due to the number of advantages. Therefore taking, the merits of herbal ingredients with drug delivery technology was developed using statistical analysis Here, the concentration of Sodium alginate, Concentration of xanthan gum, and concentration of HPMC K15 M was taken as the factors and viscosity as well as drug release (Total phenol content) in 10 h were selected as the responses The designed batch consisting of 1.711% w/v sodium alginate, 0.727% w/v xanthan gum, and 0.869% w/v HPMC K15M was selected as the optimized one as per the software and the viscosity and % drug release in 10 h were found to be 299.5cps and 70.2% respectively. Other evaluation parameters such as gelling capacity, floating parameters, and stability were also found to be good for the designed batches. The optimized in-situ gel was found to be thoughtful for extending the floating of drug incorporated in the formulation as well as residence time in the stomach for sustaining the drug release
{"title":"DoE Based Optimization of Oral In-Situ Gel Containing Dandelion Leaf Extract","authors":"M. Dholakia, Dinal Patel, Harshida Chauhan, B. Suhagia","doi":"10.2174/2210303112666220330124251","DOIUrl":"https://doi.org/10.2174/2210303112666220330124251","url":null,"abstract":"\u0000\u0000The present study developed oral in-situ gel containing the leaf extract of Taraxacum officinale (T.O.) using the Design of the experiment. Background: Peptic ulcer disease is an epidemic in the 19th and early 20th centuries. The application of herbal drugs for peptic diseases is an attractive area for research and implementation as compared to the allopathic system in the recent era. From the number of plants, the antioxidant effect of an aqueous extract of Taraxacum officinale that is Dandelion leaf was proven by an animal study in some previous literature. However, most of the marketed preparations consist root extract primarily used for detoxification of liver incomparision to the leaf extract having nonspecific application. Hence the aqueous extract of Dandelion leaf was taken as the active ingredient in the formulation. Over the past 30 years, greater attention has been focused on the development of controlled and sustained drug delivery systems. The development of in situ gel systems has received considerable attention over the past few years due to the number of advantages.\u0000\u0000\u0000\u0000Therefore taking, the merits of herbal ingredients with drug delivery technology was developed using statistical analysis\u0000\u0000\u0000\u0000Here, the concentration of Sodium alginate, Concentration of xanthan gum, and concentration of HPMC K15 M was taken as the factors and viscosity as well as drug release (Total phenol content) in 10 h were selected as the responses\u0000\u0000\u0000\u0000The designed batch consisting of 1.711% w/v sodium alginate, 0.727% w/v xanthan gum, and 0.869% w/v HPMC K15M was selected as the optimized one as per the software and the viscosity and % drug release in 10 h were found to be 299.5cps and 70.2% respectively. Other evaluation parameters such as gelling capacity, floating parameters, and stability were also found to be good for the designed batches.\u0000\u0000\u0000\u0000The optimized in-situ gel was found to be thoughtful for extending the floating of drug incorporated in the formulation as well as residence time in the stomach for sustaining the drug release\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47076004","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 : 2022-03-29DOI: 10.2174/2210303112666220329154050
Amaresh Prusty, B. K. Gupta, Amiyakanta Mishra
In this research study, an attempt has been made using Box–Behnken design (BBD) Response Surface Methodology to find optimized formulation variables at their 3 levels (Low, medium and high) to affect the dependent response which is % drug release pattern at different time intervals in extending drug release of Benidipine Hydrochloride(BH) matrix tablets. BH extended release tablets reduce the side effects associated with multiple dosing used during conventional tablets. As in the preliminary work, we have found the most profound formulation factors for extending drug release of BH matrix tablets are Eudragit RS 100 amount (X1), HPMC K 100 M (X2), chitosan amount (X3), which we selected as independent factors at their low and high levels for this study considering % drug release at three different time intervals i.e. R1 (% of drug release in 2hr), R2 (% of drug release in 15hr) and R3 (% of drug release in 18hr) as dependent variables using dissolution media of phosphate buffer pH 6.8 with 75rpm. From the experimental runs of prepared tablets as predicted by Design Expert software, the model shows a quadratic equation due to less p value, and a very less difference was observed between adjusted R2 and predicted values R2in all selected responses which we considered as % drug release. Thereforeby using the graphical response surface plot of BBD software,the optimized formulation of BH extended release tablet of Eudragit RS 100, HPMC K 100 M, Chitosan containing an amount of 45mg , 105 mg, and 45.71 mg respectively which shows an extended drug release of more than 18 hr. For constructing a satisfying fit of the model for the optimized formulation, result analysis was carried out for the internally studentized residuals versus the experimental runs indicating all data points are placed within the limits and the values of the predicted and actual response of each run were normally distributed near a straight line.
在本研究中，尝试使用Box-Behnken设计（BBD）响应面方法，在三个水平（低、中、高）上寻找优化的配方变量，以影响盐酸贝尼地平（BH）基质片在不同时间间隔的依赖性反应，即%药物释放模式。BH缓释片可减少常规片剂中多次给药的副作用。在前期工作中，我们发现延长BH基质片药物释放的最深刻的配方因素是Eudragit RS 100量（X1）、HPMC K 100 M（X2）、壳聚糖量（X3），考虑到三个不同时间间隔的药物释放%，即R1（2小时内药物释放的%），R2（15小时内药物释放的%）和R3（18小时内药物的%）作为因变量，使用pH 6.8的磷酸盐缓冲液的溶出介质，75rpm。根据Design Expert软件预测的制备片剂的实验运行，由于p值较小，该模型显示出二次方程，并且在我们认为为药物释放%的所有选择的反应中，在调整的R2和预测值R2之间观察到非常小的差异。因此，利用BBD软件的图形响应面图，对Eudragit RS 100、HPMC K 100 M、壳聚糖BH缓释片的优化处方进行了研究，其缓释量分别为45mg、105mg和45.71mg，显示出超过18小时的缓释效果，对内部学生化残差与实验运行进行了结果分析，表明所有数据点都在限制范围内，并且每次运行的预测和实际响应值正态分布在直线附近。
{"title":"Application of Box–Behnken Design Response Surface Methodology to Study Optimized Formulation Variables on Drug Release Pattern of Benidipine Hydrochloride Extended Release Matrix Tablet","authors":"Amaresh Prusty, B. K. Gupta, Amiyakanta Mishra","doi":"10.2174/2210303112666220329154050","DOIUrl":"https://doi.org/10.2174/2210303112666220329154050","url":null,"abstract":"\u0000\u0000In this research study, an attempt has been made using Box–Behnken design (BBD) Response Surface Methodology to find optimized formulation variables at their 3 levels (Low, medium and high) to affect the dependent response which is % drug release pattern at different time intervals in extending drug release of Benidipine Hydrochloride(BH) matrix tablets. BH extended release tablets reduce the side effects associated with multiple dosing used during conventional tablets.\u0000\u0000\u0000\u0000As in the preliminary work, we have found the most profound formulation factors for extending drug release of BH matrix tablets are Eudragit RS 100 amount (X1), HPMC K 100 M (X2), chitosan amount (X3), which we selected as independent factors at their low and high levels for this study considering % drug release at three different time intervals i.e. R1 (% of drug release in 2hr), R2 (% of drug release in 15hr) and R3 (% of drug release in 18hr) as dependent variables using dissolution media of phosphate buffer pH 6.8 with 75rpm.\u0000\u0000\u0000\u0000From the experimental runs of prepared tablets as predicted by Design Expert software, the model shows a quadratic equation due to less p value, and a very less difference was observed between adjusted R2 and predicted values R2in all selected responses which we considered as % drug release.\u0000\u0000\u0000\u0000Thereforeby using the graphical response surface plot of BBD software,the optimized formulation of BH extended release tablet of Eudragit RS 100, HPMC K 100 M, Chitosan containing an amount of 45mg , 105 mg, and 45.71 mg respectively which shows an extended drug release of more than 18 hr. For constructing a satisfying fit of the model for the optimized formulation, result analysis was carried out for the internally studentized residuals versus the experimental runs indicating all data points are placed within the limits and the values of the predicted and actual response of each run were normally distributed near a straight line.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41425343","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 : 2022-03-29DOI: 10.2174/2210303112666220329154123
M. Bhatia, Sunil Kumar, A. Kapoor, Sunidhi Lohan
Parasitic infections are prime causes of morbidity and mortality worldwide. Significant progress has been made to cure these infections like discovery of antiparasitic drugs, developing new formulation strategies and site-directed drug delivery and chemotherapy etc. As synthetic drugs are perilous and have various side effects leading to the development of drug resistance and loss of health. Herbal medicines are economical and generally free from potential side effects is acclaiming recognition. However, it is difficult to produce antiparasitic vaccines, major efforts have been made and still there are no licensed vaccines currently available to control human parasitic ailments. Here, a systematic review is dispensed assessing various techniques for the treatment of parasitic infections. Moreover, the advancements and challenges involved in establishing novel trends in the development of a more effective drug delivery systems are also investigated. The numbers of impending infectious ailments in humans have enhanced within the novel past or warn to increase in the future. Over thirty new infective agents have been identified globally in the last 30 years; approximately 60 % of these are from zoonotic sources. Efficient drug delivery plays a key role in treating parasitic infections. The main goal of modern antiparasitic drug delivery system is to minimize the potential side effects and bring the drug directly to the target pathogens, therefore, more sophisticated drug formulations than a simple tablet or solution are necessary for the betterment of critical situations of many human parasitic diseases.
{"title":"A review on the drug delivery strategies for parasitic infections: scope and assertion","authors":"M. Bhatia, Sunil Kumar, A. Kapoor, Sunidhi Lohan","doi":"10.2174/2210303112666220329154123","DOIUrl":"https://doi.org/10.2174/2210303112666220329154123","url":null,"abstract":"\u0000\u0000Parasitic infections are prime causes of morbidity and mortality worldwide. Significant progress has been made to cure these infections like discovery of antiparasitic drugs, developing new formulation strategies and site-directed drug delivery and chemotherapy etc. As synthetic drugs are perilous and have various side effects leading to the development of drug resistance and loss of health. Herbal medicines are economical and generally free from potential side effects is acclaiming recognition. However, it is difficult to produce antiparasitic vaccines, major efforts have been made and still there are no licensed vaccines currently available to control human parasitic ailments.\u0000\u0000\u0000\u0000Here, a systematic review is dispensed assessing various techniques for the treatment of parasitic infections. Moreover, the advancements and challenges involved in establishing novel trends in the development of a more effective drug delivery systems are also investigated.\u0000\u0000\u0000\u0000The numbers of impending infectious ailments in humans have enhanced within the novel past or warn to increase in the future. Over thirty new infective agents have been identified globally in the last 30 years; approximately 60 % of these are from zoonotic sources. Efficient drug delivery plays a key role in treating parasitic infections. The main goal of modern antiparasitic drug delivery system is to minimize the potential side effects and bring the drug directly to the target pathogens, therefore, more sophisticated drug formulations than a simple tablet or solution are necessary for the betterment of critical situations of many human parasitic diseases.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44037514","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 : 2022-03-25DOI: 10.2174/2210303112666220325112441
D. Limbasiya, Dharmik Mehta
The present study unveils a simple but innovative combination of existing treatments of three different domains with unique logical aspects. Joint pain is the major cause of disability, especially for elderly people. Currently, two widely practiced treatment options for the same are combined to produce simultaneous treatments which overcome the drawbacks of individual treatment and improve patient compliance. Moreover, a third treatment option of cooling and counterirritant material (Menthol) for pain relief was also explored successfully as a substitute treatment. In the present study, we formulated and optimized an adhesive topical patch of the model drug diclofenac sodium, a widely used medicine for pain relief and menthol, a cooling and counterirritant substance to aid pain relief. Combinations of two polymers PVP-K30 and PVA, selected by trial batches, were further optimized by applying a 3x2 full factorial design. Two factors X1 (PVP-K30) and X2 (PVA) were optimized using three responses R1 (Q2), R2 (Q4) and R3 (Q12). Derived mathematical models for responses were validated using checkpoint batches. Final optimized batch was derived based on the desirability function. Factorial batches were also evaluated for relevant parameters. Results obtained by checkpoint batches were in line with the experimental results with 5% relative error, revealing that the derived models were valid for the design. Final optimized batch obtained by desirability function followed all set criteria. Medicated patch prepared by optimized formulation was incorporated into the knee brace using in house patch holder mechanism. Combined treatment offers better patient compliance for the patient as well as the healthcare provider, which can be extended to other pain-relieving supportive treatments like elbow braces, waist brace, back support belt, cervical brace etc.
{"title":"Medicated Supportive Braces: A Synergy of Treatments for Joint Pain Relief.","authors":"D. Limbasiya, Dharmik Mehta","doi":"10.2174/2210303112666220325112441","DOIUrl":"https://doi.org/10.2174/2210303112666220325112441","url":null,"abstract":"The present study unveils a simple but innovative combination of existing treatments of three different domains with unique logical aspects. Joint pain is the major cause of disability, especially for elderly people. Currently, two widely practiced treatment options for the same are combined to produce simultaneous treatments which overcome the drawbacks of individual treatment and improve patient compliance. Moreover, a third treatment option of cooling and counterirritant material (Menthol) for pain relief was also explored successfully as a substitute treatment. In the present study, we formulated and optimized an adhesive topical patch of the model drug diclofenac sodium, a widely used medicine for pain relief and menthol, a cooling and counterirritant substance to aid pain relief. Combinations of two polymers PVP-K30 and PVA, selected by trial batches, were further optimized by applying a 3x2 full factorial design. Two factors X1 (PVP-K30) and X2 (PVA) were optimized using three responses R1 (Q2), R2 (Q4) and R3 (Q12). Derived mathematical models for responses were validated using checkpoint batches. Final optimized batch was derived based on the desirability function. Factorial batches were also evaluated for relevant parameters. Results obtained by checkpoint batches were in line with the experimental results with 5% relative error, revealing that the derived models were valid for the design. Final optimized batch obtained by desirability function followed all set criteria. Medicated patch prepared by optimized formulation was incorporated into the knee brace using in house patch holder mechanism. Combined treatment offers better patient compliance for the patient as well as the healthcare provider, which can be extended to other pain-relieving supportive treatments like elbow braces, waist brace, back support belt, cervical brace etc.","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41620325","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 : 2022-03-18DOI: 10.2174/2210303112666220318151336
A. Cetin
The COVID-19 pandemic emerged at the end of 2019 in China and spread rapidly all over the world. Scientists strive to find virus-specific antivirals against COVID-19 disease. This study aimed to assess bioactive coumarinolignans (Aquillochin, Grewin) as potential SARS-CoV-2 main protease (SARS-CoV-2 Mpro) inhibitors using a molecular docking study. The detailed interactions between the coumarinolignans and SARS-CoV-2 mpro were determined as hydrophobic bonds, hydrogen bonds and electronic bonds, inhibition activity, ligand efficiency, bonding type and distance using Autodock 4.2 software. SARS-CoV-2 Mpro was docked with Aquillochin and Grewin and the docking results were analysed by Autodock 4.2 and Biovia Discovery Studio 4.5. Nelfinavir and lopinavir were used as standards for comparison. The binding energies of the SARS-CoV-2 Mpro-coumarinolignan’s complexes were identified from the molecular docking of SARS-CoV-2 Mpro. Aquillochin and Grewin were found to be -7.5 and -8.4 kcal/mol, respectively. The binding sites of the coumarinolignans to SARS-CoV-2 Mpro were identified with the main interactions being π-alkyl, alkyl, π-cation, π-π T-Shaped and hydrogen bonding. Furthermore, SwissADME web tools were used to evaluate ADMET properties and pharmacokinetic parameters of the Aquillochin and Grewin. The results of ADMET and pharmacokinetic results of the Aquillochin and Grewin showed that these coumarinolignans were consonant with the many accepted rules and the criteria of drug likeness. Aquillochin and Grewin obey the Lipinski’s rule of five. According to the results obtained from molecular docking studies and ADMET predictions, Aquillochin and Grewin have shown weak efficacy as drug candidates against COVID-19 disease.
新冠肺炎疫情于2019年底在中国出现，并在全球迅速蔓延。科学家努力寻找针对新冠肺炎疾病的病毒特异性抗病毒药物。本研究旨在通过分子对接研究评估生物活性香豆素信号素（Aquilochin，Grewin）作为潜在的严重急性呼吸系统综合征冠状病毒2型主要蛋白酶（严重急性呼吸综合征冠状病毒2Mpro）抑制剂。使用Autodock 4.2软件确定香豆素信号素和严重急性呼吸系统综合征冠状病毒2型多聚体之间的详细相互作用为疏水键、氢键和电子键、抑制活性、配体效率、键类型和距离。严重急性呼吸系统综合征冠状病毒2型Mpro与Aquilochin和Grewin对接，Autodock 4.2和Biovia Discovery Studio 4.5对对接结果进行了分析。奈勒芬那韦和洛匹那韦被用作对照品。从严重急性呼吸系统综合征冠状病毒2型Mpro的分子对接中确定了严重急性呼吸系冠状病毒2型Mpro香豆素配体复合物的结合能。Aquilochin和Grewin分别为-7.5和-8.4千卡/摩尔。香豆素信号子与严重急性呼吸系统综合征冠状病毒2型Mpro的结合位点被鉴定，主要相互作用为π-烷基、烷基、π-阳离子、π-πT形和氢键。此外，SwissADME网络工具用于评估Aquilochin和Grewin的ADMET特性和药代动力学参数。ADMET结果和Aquilochin和Grewin的药代动力学结果表明，这些香豆素信号符合许多公认的规则和药物相似性标准。阿奎洛钦和格雷温遵守利平斯基的五人制。根据分子对接研究和ADMET预测的结果，Aquilochin和Grewin作为新冠肺炎候选药物的疗效较弱。
{"title":"Molecular Docking and Pharmacokinetic Studies of Aquillochin and Grewin as SARS-CoV-2 Mpro Inhibitors","authors":"A. Cetin","doi":"10.2174/2210303112666220318151336","DOIUrl":"https://doi.org/10.2174/2210303112666220318151336","url":null,"abstract":"\u0000\u0000The COVID-19 pandemic emerged at the end of 2019 in China and spread rapidly all over the world. Scientists strive to find virus-specific antivirals against COVID-19 disease. This study aimed to assess bioactive coumarinolignans (Aquillochin, Grewin) as potential SARS-CoV-2 main protease (SARS-CoV-2 Mpro) inhibitors using a molecular docking study.\u0000\u0000\u0000\u0000The detailed interactions between the coumarinolignans and SARS-CoV-2 mpro were determined as hydrophobic bonds, hydrogen bonds and electronic bonds, inhibition activity, ligand efficiency, bonding type and distance using Autodock 4.2 software. SARS-CoV-2 Mpro was docked with Aquillochin and Grewin and the docking results were analysed by Autodock 4.2 and Biovia Discovery Studio 4.5. Nelfinavir and lopinavir were used as standards for comparison.\u0000\u0000\u0000\u0000The binding energies of the SARS-CoV-2 Mpro-coumarinolignan’s complexes were identified from the molecular docking of SARS-CoV-2 Mpro. Aquillochin and Grewin were found to be -7.5 and -8.4 kcal/mol, respectively. The binding sites of the coumarinolignans to SARS-CoV-2 Mpro were identified with the main interactions being π-alkyl, alkyl, π-cation, π-π T-Shaped and hydrogen bonding. Furthermore, SwissADME web tools were used to evaluate ADMET properties and pharmacokinetic parameters of the Aquillochin and Grewin. The results of ADMET and pharmacokinetic results of the Aquillochin and Grewin showed that these coumarinolignans were consonant with the many accepted rules and the criteria of drug likeness.\u0000\u0000\u0000\u0000Aquillochin and Grewin obey the Lipinski’s rule of five. According to the results obtained from molecular docking studies and ADMET predictions, Aquillochin and Grewin have shown weak efficacy as drug candidates against COVID-19 disease.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47819893","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 : 2022-03-18DOI: 10.2174/2210303112666220318155445
T. Pandya, P. Bhatt, Ambikandan Misra
Obesity, considered a complex condition, is the fastest-growing public health concern worldwide. Its treatment is limited due to the side effects of pharmacological options available, outweighing their benefits. The present study aims to formulate a novel biodegradable formulation of Exenatide for direct brain delivery through the nasal route. To formulate Exenatide loaded Poly (lactide-co-glycolide) (PLGA) nanoparticles, a double emulsion (w/o/w) solvent evaporation method was employed. A full factorial (33) design of the experiment was used to optimize the formulation. The entrapment efficiency and particle size of the optimized formulation were found to be 68% and 110 nm, respectively. The in-vitro drug release study indicated the sustained release of 48% drug in 5 days. The safety of drug-loaded PLGA nanoparticles for intranasal delivery was indicated by the sheep nasal toxicity study. The efficacy of the developed nanoparticles was demonstrated by an in-vivo pharmacodynamics study on Albino wistar rats, showing a 6.2% weight reduction after 30 days of treatment. Thus, Exenatide is a novel peptide having significant weight loss benefits and no severe side effects. Long-term studies in at least two or more animal models followed by extensive clinical evaluation can safely result in a product for clinical use.
{"title":"Development and evaluation of Exenatide loaded PLGA nanoparticles for intranasal delivery in treatment of Obesity","authors":"T. Pandya, P. Bhatt, Ambikandan Misra","doi":"10.2174/2210303112666220318155445","DOIUrl":"https://doi.org/10.2174/2210303112666220318155445","url":null,"abstract":"\u0000\u0000Obesity, considered a complex condition, is the fastest-growing public health concern worldwide. Its treatment is limited due to the side effects of pharmacological options available, outweighing their benefits.\u0000\u0000\u0000\u0000The present study aims to formulate a novel biodegradable formulation of Exenatide for direct brain delivery through the nasal route.\u0000\u0000\u0000\u0000To formulate Exenatide loaded Poly (lactide-co-glycolide) (PLGA) nanoparticles, a double emulsion (w/o/w) solvent evaporation method was employed. A full factorial (33) design of the experiment was used to optimize the formulation.\u0000\u0000\u0000\u0000The entrapment efficiency and particle size of the optimized formulation were found to be 68% and 110 nm, respectively. The in-vitro drug release study indicated the sustained release of 48% drug in 5 days. The safety of drug-loaded PLGA nanoparticles for intranasal delivery was indicated by the sheep nasal toxicity study. The efficacy of the developed nanoparticles was demonstrated by an in-vivo pharmacodynamics study on Albino wistar rats, showing a 6.2% weight reduction after 30 days of treatment.\u0000\u0000\u0000\u0000Thus, Exenatide is a novel peptide having significant weight loss benefits and no severe side effects. Long-term studies in at least two or more animal models followed by extensive clinical evaluation can safely result in a product for clinical use.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42776996","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 : 2022-02-24DOI: 10.2174/2210303112666220224110100
Yashwant Giri, A. Behera, B. Mohanty, G. Pattnaik, Sk Habibullah
Onychomycosis is an infection caused by a fungus that causes discoloration and thickening of the nail layer, and it is the most common nail infection in the world. Trichophyton rubrum and Trichophyton mentagrophytes var. interdigital is the most common anthropophilic dermatophytes that trigger it. Onychomycosis is caused by yeasts such as Candida albicans and Candida parapsilosis, as well as moulds such as Aspergillus spp. Treatment is determined by the type of nail invasion, the fungus genus, and the number of nails affected. Approaches towards conventional methods showed certain drawbacks which emphasizes the need for alternate approaches to produce better therapeutic efficacy of a product. The present review focused on reporting an updated classification of Onchyomycosis, causative organisms, factors influencing drug permeation, novel treatment strategies for Onychomycosis, drug permeation enhancement methods.
{"title":"Transungual drug delivery system for the topical treatment of Onychomycosis: A review","authors":"Yashwant Giri, A. Behera, B. Mohanty, G. Pattnaik, Sk Habibullah","doi":"10.2174/2210303112666220224110100","DOIUrl":"https://doi.org/10.2174/2210303112666220224110100","url":null,"abstract":"\u0000\u0000Onychomycosis is an infection caused by a fungus that causes discoloration and thickening of the nail layer, and it is the most common nail infection in the world. Trichophyton rubrum and Trichophyton mentagrophytes var. interdigital is the most common anthropophilic dermatophytes that trigger it. Onychomycosis is caused by yeasts such as Candida albicans and Candida parapsilosis, as well as moulds such as Aspergillus spp. Treatment is determined by the type of nail invasion, the fungus genus, and the number of nails affected. Approaches towards conventional methods showed certain drawbacks which emphasizes the need for alternate approaches to produce better therapeutic efficacy of a product. The present review focused on reporting an updated classification of Onchyomycosis, causative organisms, factors influencing drug permeation, novel treatment strategies for Onychomycosis, drug permeation enhancement methods.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45372051","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 : 2022-01-27DOI: 10.2174/2210303112666220127113328
A. Nikyar, A. Bolhassani
Gene therapy is a promising approach for the treatment of various diseases including cancer, hereditary disorders, and some viral infections. Development of efficient and safe gene delivery systems is essential for facilitating gene transfer to various organs and tissues in vivo. In this review, we briefly describe the principal mechanisms of gene delivery systems, particularly electroporation, and discuss the latest advancements in the application of electroporation for in vivo gene transfer. A narrative review of all the relevant publication known to the authors was conducted. In recent years, electroporation-based strategies have emerged as an auspicious and versatile platform for efficient and controlled delivery of various biomolecules, including nucleic acids. Applying electric pulses of enough magnitude leads to the formation of hydrophilic pores in the cell membrane and allows the entry of otherwise membrane-impermeant molecules, such as DNA. Although electroporation has been initially developed for in vitro transfection of cells, it has recently advanced to preclinical in vivo applications and finally to clinical trials. Electroporation has already entered the clinical practice for antitumor therapy and may be an essential part of future personalized treatments. Given the ability of electroporation to deliver multiple genes in a single event, it will also certainly be further developed both as a stand-alone delivery approach and when coupled with other technologies.
{"title":"Electroporation: An Effective Method For In Vivo Gene Delivery","authors":"A. Nikyar, A. Bolhassani","doi":"10.2174/2210303112666220127113328","DOIUrl":"https://doi.org/10.2174/2210303112666220127113328","url":null,"abstract":"\u0000\u0000Gene therapy is a promising approach for the treatment of various diseases including cancer, hereditary disorders, and some viral infections. Development of efficient and safe gene delivery systems is essential for facilitating gene transfer to various organs and tissues in vivo.\u0000\u0000\u0000\u0000In this review, we briefly describe the principal mechanisms of gene delivery systems, particularly electroporation, and discuss the latest advancements in the application of electroporation for in vivo gene transfer.\u0000\u0000\u0000\u0000A narrative review of all the relevant publication known to the authors was conducted.\u0000\u0000\u0000\u0000In recent years, electroporation-based strategies have emerged as an auspicious and versatile platform for efficient and controlled delivery of various biomolecules, including nucleic acids. Applying electric pulses of enough magnitude leads to the formation of hydrophilic pores in the cell membrane and allows the entry of otherwise membrane-impermeant molecules, such as DNA. Although electroporation has been initially developed for in vitro transfection of cells, it has recently advanced to preclinical in vivo applications and finally to clinical trials.\u0000\u0000\u0000\u0000Electroporation has already entered the clinical practice for antitumor therapy and may be an essential part of future personalized treatments. Given the ability of electroporation to deliver multiple genes in a single event, it will also certainly be further developed both as a stand-alone delivery approach and when coupled with other technologies.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47590328","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 : 2021-10-18DOI: 10.2174/2210303111666211018115533
N. Lal, M. Rana, B. Sagar, N. Verma
Acne vulgaris is a very common skin disorder peaks at teenage, but many men and women between 20-40 years of age are also affected by the disorder. For the treatment of acne, herbal medication are considered safer than allopathic medicines as allopathic medicines are associated with side effects such as like contact allergy, local irritation, scaling, photosensitivity, itching and redness of the skin etc. The present research work was performed to check effectiveness of foaming face wash formulation containing Curcuma longa along with herbals excipient Aloe vera, Rosa centifolia and Citrus sinensis. Curcuma longa have been reported to contain active phytoconstituents having significant anti-microbial activity and used locally for acne. The plant material Curcuma longa, Aloe vera, Rosa centifolia and Citrus sinensis were authenticated and their extracts has been prepared using Soxhlet Apparatus and the the resulting essential oil was analyzed for its physical properties. The foaming face wash was than prepared by using the herbal extracts with excipients that were free from sulphates, parabens, silicon and petroleum products. Two formulations, A1and A2 has been prepared and their physicochemical studies were perfomed. The presence and efficacy of Curcuma longa in suppression of Propionibacterium acnes was assessed by analytical methods and anti-microbial techniques, respectively. Skin irritation studies were conducted using Wistar rats by scoring method. Accelerated stability studies were also performed for a period of 60 days. The physicochemical properties were evaluated and found to be satisfactory. Analytical techniques like High Performance Liquid Chromatography, High Performance Thin Layer Chromatography and Infra Red spectral analysis confirmed the qualitative presence of Curcuminoid, which is a mixture of curcumin, desmethoxycurcumin [4-hydroxycinnamoyl-(4-hydroxy-3-methoxycinnamoyl) methane] and Bis- demethoxycurcumin [bis-(4-hydroxy cinnamoyl) methane] in the sample. The Antibacterial activity of developed face wash assessed against Propionibacterium acnes was more than that of Clindamycin (10μg/ml). Also, the developed formulation showed a very high activity against Staphylococcus epidermidis with respect to the activity of the standard clindamycin. The prepared formulation showed no sign of localized reactions were confirmed by a skin irritation study indicating the formulation was safe and compatible with the skin. On the basis of our study, it could be stated, that formulation has antimicrobial activity and could be used safely on human skin
{"title":"Formulation and Standardization of Anti-Acne Herbal Foaming Face wash using Curcuma longa along with Aloe vera, Rosa centifolia and Citrus sinensis","authors":"N. Lal, M. Rana, B. Sagar, N. Verma","doi":"10.2174/2210303111666211018115533","DOIUrl":"https://doi.org/10.2174/2210303111666211018115533","url":null,"abstract":"\u0000\u0000Acne vulgaris is a very common skin disorder peaks at teenage, but many men and women between 20-40 years of age are also affected by the disorder. For the treatment of acne, herbal medication are considered safer than allopathic medicines as allopathic medicines are associated with side effects such as like contact allergy, local irritation, scaling, photosensitivity, itching and redness of the skin etc. The present research work was performed to check effectiveness of foaming face wash formulation containing Curcuma longa along with herbals excipient Aloe vera, Rosa centifolia and Citrus sinensis. Curcuma longa have been reported to contain active phytoconstituents having significant anti-microbial activity and used locally for acne. \u0000\u0000\u0000\u0000\u0000 The plant material Curcuma longa, Aloe vera, Rosa centifolia and Citrus sinensis were authenticated and their extracts has been prepared using Soxhlet Apparatus and the the resulting essential oil was analyzed for its physical properties. The foaming face wash was than prepared by using the herbal extracts with excipients that were free from sulphates, parabens, silicon and petroleum products. Two formulations, A1and A2 has been prepared and their physicochemical studies were perfomed. The presence and efficacy of Curcuma longa in suppression of Propionibacterium acnes was assessed by analytical methods and anti-microbial techniques, respectively. Skin irritation studies were conducted using Wistar rats by scoring method. Accelerated stability studies were also performed for a period of 60 days.\u0000\u0000\u0000\u0000\u0000 The physicochemical properties were evaluated and found to be satisfactory. Analytical techniques like High Performance Liquid Chromatography, High Performance Thin Layer Chromatography and Infra Red spectral analysis confirmed the qualitative presence of Curcuminoid, which is a mixture of curcumin, desmethoxycurcumin [4-hydroxycinnamoyl-(4-hydroxy-3-methoxycinnamoyl) methane] and Bis- demethoxycurcumin [bis-(4-hydroxy cinnamoyl) methane] in the sample. The Antibacterial activity of developed face wash assessed against Propionibacterium acnes was more than that of Clindamycin (10μg/ml). Also, the developed formulation showed a very high activity against Staphylococcus epidermidis with respect to the activity of the standard clindamycin. The prepared formulation showed no sign of localized reactions were confirmed by a skin irritation study indicating the formulation was safe and compatible with the skin. \u0000\u0000\u0000\u0000\u0000On the basis of our study, it could be stated, that formulation has antimicrobial activity and could be used safely on human skin\u0000\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42641196","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 : 2021-09-27DOI: 10.2174/2210303111666210927112941
R. Sekhar, Md. Shoaib Alam, Iftikhar Ahsan, S. Raja, Thusleem Mohamed, Sheikh Shafiq-un-Nabi
Conventional enteric coating is very challenging in soft gel capsules because of shell nature (smooth surfaces and elasticity). Soft gelatin capsules are highly sensitive to temperature, humidity and it can lose their tensile strength during the conventional coating process. Enteric soft gel capsules were prepared by addition of enteric polymer in the gelatin shell composition by inducing the cross linking of gelatin through chemical treatment. This dual approach makes the soft gelatin capsules to resist the drug release in stomach and reliably release their contents in the intestine within a predetermined time without affecting the physical properties of soft gel capsules. Enteric effect of soft gel capsules are brought by a specialized synergetic technique which is unique for the molecules which need intestinal drug release.
{"title":"Development of platform technology for gastro-resistant soft gel capsules by using the cross-linking technique","authors":"R. Sekhar, Md. Shoaib Alam, Iftikhar Ahsan, S. Raja, Thusleem Mohamed, Sheikh Shafiq-un-Nabi","doi":"10.2174/2210303111666210927112941","DOIUrl":"https://doi.org/10.2174/2210303111666210927112941","url":null,"abstract":"\u0000\u0000Conventional enteric coating is very challenging in soft gel capsules because of shell nature (smooth surfaces and elasticity). Soft gelatin capsules are highly sensitive to temperature, humidity and it can lose their tensile strength during the conventional coating process. \u0000\u0000\u0000\u0000\u0000 Enteric soft gel capsules were prepared by addition of enteric polymer in the gelatin shell composition by inducing the cross linking of gelatin through chemical treatment. \u0000\u0000\u0000\u0000\u0000 This dual approach makes the soft gelatin capsules to resist the drug release in stomach and reliably release their contents in the intestine within a predetermined time without affecting the physical properties of soft gel capsules.\u0000\u0000\u0000\u0000\u0000 Enteric effect of soft gel capsules are brought by a specialized synergetic technique which is unique for the molecules which need intestinal drug release.\u0000\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68161450","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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