scholarly journals Novel insight into Potential Leishmanicidal Activities of Transdermal Patches of Nigella Sativa: Formulation Development, Physical Characterizations and In vitro In vivo Assays

2021 ◽  
Author(s):  
Barkat Ali Khan ◽  
Yasmin Asmat ◽  
Tariq Hayat Khan ◽  
Mughal Qayum ◽  
Sultan Muhammad Alshahrani ◽  
...  
Keyword(s):  
Drug Release ◽  
Nigella Sativa ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
Formulation Development ◽  
Standard Drug ◽  
Drug Permeation ◽  
Transdermal Patches

Abstract Cutaneous Leishmaniasis (CL) is the most common type of Leishmaniasis which annually affects 1.5 million people worldwide. About 90% of cases are reported from countries such as Iran, Afghanistan, Pakistan, Iraq, and Saudi Arabia. The purpose of the present study was to fabricate transdermal patches of Nigella sativa (NS), characterize and to check its in vitro in vivo anti-Lieshmanial activity. Hydroalcohlic extract was analyzed for preliminary phytochemicals. Five formulations of transdermal patches (NS1, NS2, NS3, NS4 and NS5) were prepared by solvent evaporation method. The optimized formulation NS5 was characterized for FTIR, smoothness, brittleness, clarity, thickness, folding endurance, uniformity of weight, percent moisture content, in-vitro drug release, release kinetics, ex vivo drug permeation and in-vitro anti-Lieshmanial activity. In vivo anti-Lieshmanial activity was assessed in 30 patients (n = 30) suffering from CL. The FTIR studies showed no incompatibility among the active extract and polymers. In vitro anti-Lieshmanial assay was 194.6 ± 1.88 % as compared to standard drug (p > 0.05) and in vivo anti-Lieshmanial activity was 75 %. The drug release after 24 hours was 87.0 ± 0.94% in NS5 which showed non-Fickian diffusion mechanism while drug permeation across rabbit skin after 24 hours was up to 80.0 ± 0.91%. The results concluded that problems related to the medications parenterally used for Lieshmanial treatment can be managed by applying extract of Nigella sativa seeds in the form of transdermal patch.

scholarly journals FORMULATION DEVELOPMENT AND IN VITRO EVALUATION OF ALENDRONATE BUCCAL TABLETS

2019 ◽  
Vol 9 (4-s) ◽  
pp. 363-369
Author(s):  
SANJAY KUMAR GUPTA ◽  
Sradhanjali Patra ◽  
Syed Adnan Akber
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Ethyl Cellulose ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
Extensive Literature ◽  
Formulation Development ◽  
Alendronate Sodium ◽  
Buccal Tablets

The aim of this work was to develop a mucoadhesive buccal tablet for the buccal delivery of the alendronate via buccal mucosa. Buccal tablets of alendronate are designed to release drug at mucosal site for extended period of time without wash out of drug by saliva. Alendronate sodium is a bisphosphonates which has antiresorptive effect which is implicated in the prophylaxis and treatment of osteoporosis. Sodium alginate, ethyl cellulose and carbopol were selected as mucoadhesive polymers on the basis of their matrix forming properties. The objective of the study is to improve the bioavailability of alendronate buccal tablets. Extensive literature survey was done for the collection of theoretical and technical data. The methodology part includes the explanation of implemented methods in the present study. In present study, an attempt was made to design mucoadhesive buccal tablets containing alendronate, sodium alginate, ethyl cellulose and carbopol using as polymers. The tablets were prepared by direct compression method. The formulations were evaluated for hardness, thickness, friability, weight variation, drug content estimation, surface pH determination, swelling index, in vitro drug release. In vitro bioadhesive strength & in vitro release studies showed that formulation F11 showed optimum bioadhesive & exhibited optimum drug release 97.6% in 7hr. Kinetics results reveals that the F11 formulation follows zero order kinetics as correlation coefficient (r2) values are higher than that of first- order release kinetics.Optimized formula F11 show drug is released by non-Fickian diffusion mechanism. The stability studies of formulation F11 prepared mucoadhesive buccal tablets of alendronate were stable. Overall evaluations of the mucoadhesive of tablets show good mucoadhesive properties.

scholarly journals DILTIAZEM HCL MICROCAPSULES USING ETHYL CELLULOSE ETHER DERIVATIVE POLYMER AS RELEASE RETARDING AGENT: IN-VITRO CHAPTER

2015 ◽  
Vol 3 (8) ◽  
pp. 78-93
Author(s):  
KifayatUllah Shah ◽  
Gul Majid Khan ◽  
ShefaatUllah Shah ◽  
Asim Ur Rehman ◽  
Abdul Wahab ◽  
...  
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Angle Of Repose ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Cellulose Ether ◽  
Tap Density ◽  
Diltiazem Hcl

This study presents sustained releasemicroencapsulation of Diltiazem HCL. Its in-vitro dissolution study in phosphate buffer pH 7.4 as dissolution medium and in vivo behaviour in animal subjects. The microcapsules were prepared using polymers Ethocel 7P and Ethocel 7FP at two different drug to polymer (D: P) ratios i.e. 1:5 and 1:10 and the effect of concentration was observed on drug release behaviour. The prepared microcapsules were evaluated for different physical characteristics i.e. Bulk density, Tap density, Compressibility index, Hausner’s ratio and Angle of repose. Characterization of the developed microcapsules was carried out using Differential Scanning Calorimetery and Fourier Transform Infrared Spectroscopy while Scanning Electron Microscopy was performed to observe the morphology of the microcapsules. Model dependent and in dependent approaches were used to find out the drug transport mechanism and to compare the drug release profiles with standard formulation respectively. All the formulations show anomalous, non-Fickian diffusion mechanism and the data was best fitted in Korsmeyer’sPeppas equation. While carrying out in vivo studies, simple and rapid HPLC methods were developed which revealed optimum serum concentration (Cmax) levels for the developed microcapsules predicting least chances of side or adverse effects.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Formulation development of folic acid conjugated PLGA nanoparticles for improved cytotoxicity of Caffeic acid phenethyl ester

2021 ◽  
Vol 09 ◽  
Author(s):  
Harshad S Kapare ◽  
Sathiyanarayanan L ◽  
Arulmozhi S ◽  
Kakasaheb Mahadik
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Therapeutic Effects ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Active Constituent

Background: Honey bee propolis is one of the natural product reported in various traditional systems of medicines including Ayurveda. Caffeic acid phenethyl ester (CAPE) is an active constituent of propolis which is well known for its anticancer potential. The therapeutic effects of CAPE are restricted owing to its less aqueous solubility and low bioavailability. Objective: In this study CAPE loaded folic acid conjugated nanoparticle system (CLFPN) was investigated to enhance solubility, achieve sustained drug release and improved cytotoxicity of CAPE. Methods: Formulation development, characterization and optimization were carried out by design of experiment approach. In vitro and in vivo cytotoxicity study was carried out for optimized formulations. Results: Developed nanoparticles showed particle size and encapsulation efficiency of 170 ± 2 - 195 ± 3 nm and 75.66 ± 1.52 - 78.80 ± 1.25 % respectively. Optimized formulation CLFPN showed sustained drug release over a period of 42 h. GI50 concentration was decreased by 46.09% for formulation as compared to CAPE in MCF-7 cells indicating targeting effect of CLFPN. An improved in vitro cytotoxic effect was reflected in in-vivo Daltons Ascites Lymphoma model by reducing tumor cells count. Conclusion: The desired nanoparticle characteristic with improved in vivo and in vitro cytotoxicity was shown by developed formulation. Thus it can be further investigated for biomedical applications.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Design and Characterization of Combinational Domperidone-Famotidine Floating Drug Delivery System - In vitro and In vivo studies

2021 ◽  
Vol 62 (2) ◽  
pp. 144-162
Author(s):  
Mounika Chidurala ◽  
Raveendra Reddy J
Keyword(s):  
Drug Release ◽  
Oral Administration ◽  
Quality By Design ◽  
Release Kinetics ◽  
Cost Effective ◽  
Fickian Diffusion ◽  
In Vivo Studies ◽  
Pharmacokinetic Studies

Introduction: The drawbacks assosiated with oral administration of drugscan be controlled or minimized by gastro retentive formulations that remain buoyant within the stomach for an extended time by providing prolonged gastric retention and releasethe drug in an exceedingly extended manner thereby improving bioavailability. The current research was to develop and optimize Domperidone and Famotidine floating tablets with extended release by Quality by Design approach. Method: Based on QTPP (Quality Target Product Profile), CQAs (Critical Quality Attributes)wereidentified. Risk analysis by the evaluation of formulation and process parameters showed that optimizing the levels of polymers could reduce high risk to achieve the target profile. A 23factor experimental design with midpoints was selected for statistical analysis and optimization. Results: HPMC K100 and Carbopol 934P had a positive effect while ethyl cellulose demonstrated a negative effect on the selected responses. Drug release kinetics followed the first-order release with Higuchi diffusion and Fickian diffusion. Optimized formula satisfying all the required parameters was selected and evaluated. The predicted response values were in close agreement with experimental response values. Abdominal X-ray imaging after oral administration of the tablets on a healthy rabbit’s stomach confirmed the extended floating behavior with shorter lag time. In vivo, pharmacokinetic studies in rabbits revealed that the optimized formulation exhibited prolonged drug release with enhanced Cmax, tmax, AUCo-t, and t1/2 of an optimized product when compared to the marketed product. Conclusions: It has been concluded that the application of Quality by Design in the formulation and optimization reduced the number of trials to produce a cost-effective formula.

Quality by Design enabled anti-hypertensive Floating drug delivery system by Risk assessment and Design of Experiment (DoE) – In vitro – In vivo correlation studies

2021 ◽  
Vol 16 ◽  
Author(s):  
Mounika Chidurala ◽  
Raveendra Reddy J
Keyword(s):  
Drug Release ◽  
Risk Analysis ◽  
Quality By Design ◽  
Release Kinetics ◽  
Cost Effective ◽  
Fickian Diffusion ◽  
In Vivo Studies ◽  
Pharmacokinetic Studies

Background: The present research aimed to develop and optimize extended-release floating tablets of Sacubitril and Valsartan through Quality by Design (QbD) approach. Risk analysis by formulation assessment and process parameters showed that optimizing the levels of the polymer will minimize high risk to meet the target profile. A two (2) level three (3) full factorial experimental design along with midpoints was carefully chosen for optimization and statistical analysis. Based on the literature, the independent and dependent variables were selected. Results: HPMC K100, Carbopol 934P had a positive effect, whereas Ethylcellulose had a negative effect on Floating time, drug release at 2 h, drug release at 12 h and, 50% responses. Drug release kinetics followed the first-order release with Higuchi and Fickian diffusion. Contour and overlay plots were utilized for an assortment of design space and optimized formula. ANOVA results of all the factors exhibited significance at p<0.05. Abdominal X-ray imaging of the optimized tablets on healthy rabbit’s stomach confirmed the floating behavior for more than 12 h. In vivo pharmacokinetic studies in rabbits showed that the optimized formulation exhibited prolonged and extended drug release with improved Cmax, tmax, AUCo-t, and t1/2 of test product when compared to marketed product. IVIVC model was developed by using dissolution data of in vitro and pharmacokinetics data of in-vivo by de-convolution method (Wagner-Nelson method). Conclusion: The Quality by Design implementation in the formulation and optimization abridged the number of trials to produce a cost-effective formula. In vivo studies confirmed that the formula was successfully developed with extended floating time (12 h) and drug release by risk analysis and experimental designs. Level A correlation was observed which confirmed a good correlation between in vitro and in vivo data.

scholarly journals DESIGN AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PHENFORMIN HYDROCHLORIDE

2017 ◽  
Vol 9 (6) ◽  
pp. 90
Author(s):  
Pratik Swarup Das ◽  
Puja Saha
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Chemical Properties ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Transdermal Patches ◽  
The Matrix

Objective: In present work was designed to develop suitable transdermal matrix patches of Phenformin hydrochloride using various hydrophilic (HPMC) and hydrophobic (EUDRAGID) polymers as matrix formers.Methods: Transdermal patches containing Phenformin hydrochloride were prepared by the solvent casting evaporation technique.Results: Revealed that prepared patches showed good physical characteristics, no drug-polymer interaction and no skin irritation was observed. The in vitro release study revealed that F3 formulation showed maximum release in 24 h. Formulation F3 was subjected for accelerated stability studies. The F3 formulation was found to be stable as there was no drastic change in the Physico-chemical properties of the patches, which was also confirmed by FTIR.Conclusion: Thus conclusion can be made that stable transdermal patches of Phenformin hydrochloride has been developed. F1, F2, F3, F4 formulations showed highest cumulative percentage drug release of 98.13%, 95.50%, 98.65%, 97.21% were obtained during in vitro drug release studies after 24 h. The release of Phenformin hydrochloride appears to be dependent on lipophilicity of the matrix. Moderately lipophillic matrices showed best release. The predominant release mechanism of drug through the fabricated matrices was believed to be by diffusion mechanism. Based upon the in vitro dissolution data the F3 formulation was concluded as optimized formulation.

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