Allopurinol Loaded Transferosomes for the Alleviation of Symptomatic After-effects of Gout: An Account of Pharmaceutical Implications

2020 ◽  
Vol 15 (4) ◽  
pp. 404-419
Author(s):  
Ruchi Tiwari ◽  
Gaurav Tiwari ◽  
Rachna Singh
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vivo Studies ◽  
Transdermal Drug Delivery System

Background: The present study assessed the transdermal potential of transferosomes loaded with allopurinol for the treatment of gout. Methods: Transferosomes of allopurinol were composed of different ratios of tween-80, soya lecithin and solvent using a thin-film hydration method. Transferosomes were characterized for Scanning Electron Microscopy (SEM), zeta potential, % entrapment efficiency (%EE), Fourier Transform Infrared Spectroscopy (FTIR), in-vitro drug release and kinetics as well as stability. Then, optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, ex vivo skin permeation study, flux, and stability. Results: SEM studies suggested that vesicles were spherical and zeta potential were in the range of -11.4 mV to -29.6 mV and %EE was 52.4- 83.87%. FTIR study revealed that there was no interaction between allopurinol and excipients during the preparation of transferosomes. The cumulative percentage of drug release from various transferosomes was ranged from 51.87 to 81.87%. A transferosomal gel of F8 formulation was prepared using dispersion method reported pseudoplastic rheological behavior, optimum pH, spreadability and maximum drug permeation i.e. 79.84% with flux 13.06 g/cm2/hr, followed zero-order release kinetics. Irritation and in-vivo studies of optimized transferosomal gel G8 on rabbits revealed better results than the standard allopurinol. Conclusion: This research suggested that allopurinol loaded transferosomal gel can be potentially used as a transdermal drug delivery system for the treatment of gout.

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

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 Development and Optimization of Proniosomal Gel Containing Etodolac: In-vitro, Ex-vivo and In-vivo Evaluation

2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
In Vivo Evaluation ◽  
Vesicle Size ◽  
Skin Delivery ◽  
The Stability

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.

scholarly journals Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1218
Author(s):  
Mohammad A. Altamimi ◽  
Afzal Hussain ◽  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Usamah Abdulrahman Alnemer
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Oral Drug ◽  
In Vitro Drug Release ◽  
Drug Deposition ◽  
Drug Content

Introduction: Luteolin (LUT) is natural flavonoid with multiple therapeutic potentials and is explored for transdermal delivery using a nanocarrier system. LUT loaded cationic nanoemulsions (CNE1–CNE9) using bergamot oil (BO) were developed, optimized, and characterized in terms of in vitro and ex vivo parameters for improved permeation. Materials and methods: The solubility study of LUT was carried out in selected excipients, namely BO, cremophor EL (CEL as surfactant), labrasol (LAB), and oleylamine (OA as cationic charge inducer). Formulations were characterized with globular size, polydispersity index (PDI), zeta potential, pH, and thermodynamic stability studies. The optimized formulation (CNE4) was selected for comparative investigations (% transmittance as %T, morphology, chemical compatibility, drug content, in vitro % drug release, ex vivo skin permeation, and drug deposition, DD) against ANE4 (anionic nanoemulsion for comparison) and drug suspension (DS). Results: Formulations such as CNE1–CNE9 and ANE4 (except CNE6 and CNE8) were found to be stable. The optimized CNE4 based on the lowest value of globular size (112 nm), minimum PDI (0.15), and optimum zeta potential (+26 mV) was selected for comparative assessment against ANE4 and DS. The %T values of CNE1–CNE9 were found to be ˃95% and CEL content slightly improved the %T value. The spherical CNE4 was compatible with excipients and showed % total drug content in the range of 97.9–99.7%. In vitro drug release values from CNE4 and ANE4 were significantly higher than DS. Moreover, permeation flux (138.82 ± 8.4 µg/cm2·h), enhancement ratio (8.23), and DD (10.98%) were remarkably higher than DS. Thus, ex vivo parameters were relatively high as compared to DS which may be attributed to nanonization, surfactant-mediated reversible changes in skin lipid matrix, and electrostatic interaction of nanoglobules with the cellular surface. Conclusion: Transdermal delivery of LUT can be a suitable alternative to oral drug delivery for augmented skin permeation and drug deposition.

DESIGN OF PRONIOSOMAL GEL CONTAINING EUGENOL AS AN ANTIFUNGAL AGENT FOR THE TREATMENT OF ORAL CANDIDIASIS

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (09) ◽  
pp. 55-57
Author(s):  
T. S Vishnu ◽  
◽  
A. Dubey ◽  
G.S Ravi ◽  
S. Hebbar
Keyword(s):  
Antifungal Activity ◽  
Drug Release ◽  
Release Kinetics ◽  
Oral Candidiasis ◽  
In Vivo Studies ◽  
Compatibility Study ◽  
In Vitro Drug Release ◽  
Release Study

The objective of this study was to design and investigate the antifungal activity of proniosomal gel of eugenol for the treatment of oral candidiasis. The proniosomal gel was prepared by coacervation phase separation method using different surfactants like spans 20, 60, 80, soya lecithin and cholesterol. The proniosomal gel formulations were evaluated for visual inspection, pH detection, viscosity, spreadability, in vitro drug release and kinetics study, and in vivo studies. The compatibility study indicated that the drug and the excipients were compatible with each other. The results showed that pH, viscosity and spreadability were all acceptable for topical preparation. In vitro drug release study and drug release kinetics were conducted to check the release study and drug release patterns of the formulation. Amongst the formulations, an optimized formulation was selected to conduct an in vivo study. Candida albicans was used to induce oral candidiasis for the evaluation of therapeutic efficacy of proniosomal gel in immunosuppressed rats. Activity was analysed by microbiological and histopathological techniques and was compared with the marketed product. It is evident from the study that the proniosomal gel shows sustained release trend with strong antifungal activity.

In vitro and In vivo Evaluation of Propranolol Microspheres Loaded Buccal Gel

2017 ◽  
Vol 10 (2) ◽  
pp. 3661-3668
Author(s):  
Gajanan J Deshmukh ◽  
M. Mohan Varma ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Ex Vivo ◽  
Fickian Diffusion ◽  
In Vivo Studies ◽  
In Vivo Evaluation ◽  
Mechanical Stirring ◽  
Zero Order Kinetics

The selected propranolol microsphere formulation, S6 was employed for gel formulation with a variety of polymers like Carbopol 934, HPMC and Sodium CMC by mechanical stirring method in order to develop a sustained release propranolol microspheres containing bioadhesive gel. The prepared bioadhesive gels were evaluated for pH, viscosity, %drug content, in vitro drug release studies, bioadhesion, ex vivo permeation studies, accelerated stability and in vivo bioavailability studies. From all the above studies FG3 was found to be optimized formulation. In vitro experiments indicated a sustained release of 98.92% over 12 h and an acceptable bioadhesion quality for formulation FG3. Optimized formulation was characterized for FTIR, SEM and stability studies and found to be stable. Propranolol Optimized formulation exhibited significant increased bioavailability in vivo when compared with marketed tablet. The drug release from the optimized formulation follows zero order kinetics with anomalous Non-fickian diffusion. In vivo studies revealed that Propranolol Optimized formulation FG3 exhibited significant increased bioavailability when compared with marketed product, due to reduced first pass metabolism, when it is administered by the buccal route. Hence, it can be concluded that the formulation FG3 has potential to deliver Propranolol in a controlled and constant manner for prolong period over other formulations and can be adopted for a successful delivery of propranolol for buccal use.

scholarly journals Enhancement of the Anti-inflammatory Efficacy of Betamethasone Valerate via Niosomal Encapsulation

2021 ◽  
Vol 11 (6) ◽  
pp. 14640-14660
Keyword(s):  
Zeta Potential ◽  
Rheological Behavior ◽  
Ex Vivo ◽  
Histopathological Examination ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Betamethasone Valerate ◽  
In Vivo Studies ◽  
Anti Inflammatory

Betamethasone valerate-loaded niosomes were formulated to improve drug anti-inflammatory efficacy and reduce its systemic side effects by providing prolonged and localized drug delivery into the skin. Niosomes were prepared by thin-film hydration using different molar ratios of surfactant, cholesterol, and charge inducers. Formulations were characterized for entrapment efficiency, morphology, size, and zeta potential. In-vitro release and stability studies were conducted on selected formulations. Two niosomal gels were evaluated for spreadability, pH, rheological behavior, ex-vivo skin permeation, and in-vivo anti-inflammatory efficacy. Formulations showed high encapsulation efficiency reaching 92.03±1.88%. Vesicles were spherical in shape, ranging from 123.1 to 782 nm, and had large negative values of zeta-potential. They showed a biphasic release pattern which was more sustained than free drug suspension. Niosomes demonstrated good physicochemical stability under refrigeration for up to 3 months. Niosomal gels exhibited good spreadability, suitable pH values, favorable rheological behavior, and higher skin permeation than the plain gel. In-vivo studies revealed that niosomal gels showed a better sustained anti-inflammatory effect than drug plain gel and the marketed product, which was confirmed by further histopathological examination of paw tissues. Niosomal gels are promising formulations for sustained local delivery of betamethasone valerate.

FORMULATION AND EVALUATION OF MICROSPHERES FOR NASAL DELIVERY OF ANTI-HYPERTENSIVE DRUG

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (10) ◽  
pp. 21-26
Author(s):  
S. S Shelake ◽  
◽  
R. M Mhetre ◽  
S. V Patil ◽  
S. S Patil ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Nasal Delivery ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Hypertensive Drug

Lisinopril is used in the treatment of hypertension and heart failure in myocardial infarction and also in diabetic nephropathy. It is very poorly absorbed from GIT. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers may provide a significant increase in the nasal residence time. The microspheres prepared by emulsion solvent evaporation method were characterized for encapsulation efficiency, drug loading, particle size, surface morphology, degree of swelling, ex vivo mucoadhesion, drug release and ex vivo diffusion studies. Entrapment efficiency of microspheres was in range of 84.95±0.50% to 97.44±0.61% mucoadhesion was 83.76% and 94.41% and drug release up to 40 minutes was 53.66% to 88.32%. In ex vivo studies, the microspheres showed good bioavailability by nasal route compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres are better than single carbopol-based formulation for the delivery of lisinopril.

Quercetin Loaded Nanostructured Lipid Carriers-based Gel for Rheumatoid Arthritis: Formulation, Characterization and in vivo Evaluation

2018 ◽  
Vol 11 (1) ◽  
pp. 3967-3977
Author(s):  
Jayanti P Gokhale ◽  
Sanjay S Surana
Keyword(s):  
Rheumatoid Arthritis ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Blood Cells ◽  
Ex Vivo ◽  
In Vitro Drug Release ◽  
Texture Profile

Present research work describes the development of potential topical treatment containing nanostructured lipid carriers (NLCs) for rheumatoid arthritis (RA). Quercetin (QCT) is a renowned flavonol useful as model drug for carriers. QCT loaded NLCs were prepared and evaluated for particle size distribution, polydispersity index, zeta potential analysis, in vitro drug release study. Ex vivo study was carried out to evaluate the effect of NLCs on cell proliferation (HIG-82 cell line) and inflammation (TNF-α induction in RAW264.7 cells). The QCT-NLCs showed mean particle size of 155.6 ± 1.8 nm and polydispersity index (PDI) was 0.236 ± 0.4, entrapment efficiency of 95.63 ± 0.14 % and zeta potential of -27 ± 1.2 mV. For the ease of application, NLCs were incorporated into the gel base and final formulation was evaluated for rheological study, texture profile, drug release and antiarthritic activity. QCT-NLC gel showed pseudo plastic flow behavior with excellent texture profile parameters. In vitro drug release studies showed that, QCT-NLC gel has more prominent permeation profile as compared with QCT-loaded gel. In vivo activity was carried out using Complete Freund's adjuvant (CFA) induced arthritic model. Evaluation of the severity of rheumatoid arthritis was done by measurements of hind paw volume, arthritis score and haematological parameters such as rheumatoid factor (RF), C-reactive protein (CRP), red blood cells (RBCs), white blood cells (WBCs), erythrocyte sedimentation rate (ESR) and hemoglobin (Hb). Edema and erythema were not observed after administration of QCT-NLC- gel on the rat skin. In conclusion, the results of in vitro and ex vivo studies, QCT-NLC gel appears a viable formulation system for topical delivery of QCT in the treatment of RA.         

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