Formulation and evaluation of Cassia tora phytosomal gel using central composite design.

2021 ◽  
Vol 14 ◽  
Author(s):  
Leander Corrie ◽  
Raghunandan Gundaram ◽  
Latha Kukatil
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Therapeutic Activity ◽  
In Vitro Drug Release ◽  
Cassia Tora ◽  
Dependent Variables ◽  
Antifungal Effects ◽  
Two Parameters ◽  
Central Composite

Background:: Cassia tora has been classified as an antifungal agent, but no optimized formulation for improved drug penetration has been developed. Objective:: The present work aimed to formulate Cassia tora extract (CTE) phytosomal gel that could be used for its antifungal effects and improved therapeutic activity. Materials and Methods: The CTE phytosomes were formulated by varying the concentration of lecithin (0.15-0.25% w/v) and speed of rotation (100-160 rpm). A 22 factorial design was applied by taking the above two parameters as independent variables and vesicular size and entrapment efficiency as dependent variables. The phytosomes were also evaluated for polydispersity index, zeta potential and in vitro drug release. The optimized phytosomes of CTE were further developed into a gel, the optimized gel was also evaluated and stability studies were conducted. Results and Discussion: The optimized CTE phytosome showed a vesicular size of ~ 124 nm and entrapment efficiency of 95%. The CTE phytosomes showed a drug release of 58.79% in 24 hours following Higuchi's order of release. The CTE phytosomes were formulated into a gel by using 1% Carbopol 934 and were evaluated for pH, viscosity and homogeneity. The formulated gel showed better penetration than conventional gel and stability changes indicated no major changes to the CTE phytosomal gel. Conclusion: The optimized gel had better penetration and drug release than the conventional gel. Its therapeutic activity, therefore can be estimated to be enhanced.

scholarly journals Development and Evaluation of Clove and Cinnamon Supercritical Fluid Extracts-Loaded Emulgel for Antifungal Activity in Denture Stomatitis

Gels ◽  
2022 ◽  
Vol 8 (1) ◽  
pp. 33
Author(s):  
Meenakshi Srinivas Iyer ◽  
Anil Kumar Gujjari ◽  
Sathishbabu Paranthaman ◽  
Amr Selim Abu Lila ◽  
Khaled Almansour ◽  
...  
Keyword(s):  
Drug Release ◽  
Cure Rate ◽  
In Vitro Drug Release ◽  
Promising Alternative ◽  
Denture Stomatitis ◽  
Antifungal Effects ◽  
The Common ◽  
Central Composite

Denture stomatitis (DS), usually caused by Candida infection, is one of the common denture-related complications in patients wearing dentures. Clove and cinnamon oils have been acknowledged for their anti-inflammatory, antimicrobial activity, and antifungal effects in the oral cavity. The aim of this study, therefore, was to prepare clove/cinnamon oils-loaded emulgel and to assess its efficacy in treating Candida albicans-associated denture stomatitis. Central composite design was adopted to formulate and optimize clove/cinnamon extracts-loaded emulgel. The formulated preparations were assessed for their physical appearance, particle size, viscosity, spreadability, and in-vitro drug release. In addition, in-vivo therapeutic experiments were conducted on 42 patients with denture stomatitis. The prepared emulgel formulations showed good physical characteristics with efficient drug release within 3 h. In addition, in-vivo antifungal studies revealed that the optimized formula significantly (p < 0.001) reduced Candida colony counts from the denture surface, compared to commercially available gel (240.38 ± 27.20 vs. 398.19 ± 66.73 CFU/mL, respectively). Furthermore, the optimized formula and succeeded in alleviating denture stomatitis-related inflammation with a better clinical cure rate compared to commercially available gel Collectively, herbal extracts-loaded emulgel might be considered an evolution of polyherbal formulations and might represent a promising alternative to the existing allopathic drugs for the treatment of denture stomatitis, with better taste acceptability and no side effects.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

Formulation and Evaluation of Luliconazole Microsponges Loaded Gel for Topical Delivery

2021 ◽  
pp. 5775-5780
Author(s):  
Farhana Sultan ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Production Yield ◽  
In Vitro Drug Release ◽  
Eudragit Rs ◽  
Diffusion Studies

Microsponge containing Luliconazole (LCZ) with different proportion of drug:polymer (Ethyl cellulose and Eudragit RS 100) were obtained efficiently using Quasi-emulsion solvent diffusion method. Luliconazole is an anti-fungal drug used for the topical delivery. The purpose of the microsponge formulation is to control the release of LCZ drug to the skin through Microsponge Delivery System (MDS) known to be the novel technique which overcome the maximum concentration of active ingredient, frequency doses, and skin irritation. The prepared microsponges were examined using drug content, % production yield, % entrapment efficiency and in-vitro drug release. The formulation were subjected to in-vitro drug release studies for 6 hr in which it was concluded that Ethyl cellulose microsponges formulated by drug:polymer (1:1) and Eudragit RS 100 microsponges formulated by drug:polymer (1:3) showed maximum controlled release i.e., Increase in drug:polymer ratio (1:1 to 1:9) increased the production yield and entrapment efficiency of microsponges using Ethyl cellulose with no significant effect for Eudragit RS 100.Therefore, both formulation F1 and F2 was dispersed in carbopol gel preparation for controlled delivery of LCZ to the skin. Various physical parameters like pH, spreadability, viscosity and in-vitro drug diffusion studies were evaluated for the prepared gel formulations. Microsponge gel formulation i.e., FG1 showed better results for controlled release of 89.40% as compared to FG2 i.e., 92.18% over the period of 12 hrs which is performed in Franz Diffusion Cell. On basis of in-vitro diffusion studies for LCZ gel formulation, microsponges using Ethyl cellulose (FG1) was found to be best for its controlled release of LCZ for 12 hrs and followed zero order kinetics. Hence, formulated LCZ loaded gel have potential to treat fungal infections i.e., tinea pedis, tinea cruris and tinea corporis.

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 DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Development and In-Vitro Evaluation of Budesonide Mucoadhesive Microspherefor Pulmonary Drug Delivery

2021 ◽  
Vol 11 (2-S) ◽  
pp. 76-81
Author(s):  
Jddtadmin Journal
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Chemical Interaction ◽  
Entrapment Efficiency ◽  
Pulmonary Drug Delivery ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.   Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.

scholarly journals FORMULATION, DEVELOPMENT AND CHARACTERISATION OF NIMODIPINE LOADED SOLID LIPID NANOPARTICLES

2020 ◽  
pp. 265-271
Author(s):  
REMYA P. N. ◽  
DAMODHARAN N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Stearic Acid ◽  
Palmitic Acid ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release

Objective: The aim of the present study is to develop solid lipid nanoparticles (SLNs) of Nimodipine using hot homogenization followed by ultrasonication technique and to improve the dissolution characteristics of the drug. Methods: The Nimodipine-loaded SLN was prepared using palmitic acid and stearic acid as a lipid matrix and Tween-80 as an emulsifier by a hot homogenization and ultra-sonication method. The physicochemical characteristics of SLN were investigated for entrapment efficiency, zeta potential, in vitro drug release, particle size analysis, Fourier transform infrared studies, scanning electron microscopy, and stability studies. Results: The mean particle size, PDI, Zeta potential and entrapment efficiency of optimized Nimodipine SLN formulation of stearic acid was found to be 119.54 nm, 0.165,-17.60mV, 85% and for palmitic acid was found to be 132.54 nm, 0.155,-17.0mV, 81% respectively. In vitro drug release studies indicated that after an initial burst release, SLN could provide prolonged release of Nimodipine. The selected SLNs have shown good stability for a period of 180 d. Conclusion: SLN formulations showed the best results in EE as well as in vitro drug release and therefore, these results indicate that SLN might be a promising delivery system to enhance the release of Nimodipine.

scholarly journals Enhancement and Extended Release of the Anti-hypertensive Drug Carvedilol using Optimized Ethosomal Gel via Transdermal Route

2020 ◽  
Author(s):  
Padmanabha Rao Amarachinta ◽  
Noufel Samed ◽  
Ananda Kumar Ch. ◽  
Madhusudhan Alle ◽  
Jin-Chul Kim
Keyword(s):  
Drug Release ◽  
Transdermal Delivery ◽  
Physical Appearance ◽  
Entrapment Efficiency ◽  
Hepatic Metabolism ◽  
In Vitro Drug Release ◽  
Rapid Action ◽  
Alternative Drug ◽  
Hypertensive Drug

Abstract BackgroundCarvedilol, a popular anti-hypertensive drug, when orally administered has very poor bioavailability on the account of undergoing hepatic metabolism and therefore it becomes primal to explore an alternative drug delivery route for carvedilol. For a drug to be delivered by undergoing the least number of stages of metabolism and achieve high target specificity, transdermal delivery is the most preferred route. Hence, a study was conducted to test the potential of ethosomes as a candidate for transdermal delivery of carvedilol. A statistical study by using Central Composite Design (CCD) was also conducted for optimizing the quantity of the primary constituents present in the ethosomes. The optimized ethosomal formulation was then incorporated into a hydrogel to prepare the ethosomal gel.ResultsThe optimized formulated ethosomal suspension and the ethosomal gel were undergone physicochemical, compatibility and in-vitro drug release studies along with characterization studies. The incorporation of the ethosomes into the hydrogel proved to be effective for skin application thereby ensuring better transdermal delivery. The optimized ethosomal gel has showed credible physical appearance, spreadability, viscosity and in-vitro drug release. The pharmacodynamic studies conducted on Wister rats revealed that the anti-hypertensive action was gradual and sustained lasting up to a period of 24 hours. The stability studies conducted also showed that prepared formulations maintained its consistency within the range for the measured parameters of physical appearance, rheological properties and entrapment efficiency for a period of 3 months.Conclusions The incorporation of the drug loaded into hydrogel and its effect on regulating systolic blood pressure in a sustained way lasting 24 hours proved to be better than the present available marketed formulation which has a rapid action with the anti-hypertensive effect lasting only for 10 hours. The chosen route for delivering the drug transdermally hence proved to be effective with better enhancement and permeation capability and shows the high potential of ethosomes to be considered for novel delivery of other anti-hypertensive drugs.

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