Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release

Gojjala Venugopalarao,1 Rajasekhar Lakshmipathy,2 Nallani Chakravarthula Sarada1 1Environmental and Analytical Chemistry Division, School of Advanced Sciences, VIT University, Vellore, 2Centre for Material Science, KCG College of Technology, Chennai, India Background: The application of a...

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Autores principales: Venugopalarao G, Lakshmipathy R, Sarada NC
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Publicado: Dove Medical Press 2015
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spelling oai:doaj.org-article:e77f0be73c32467e81138cea0233d8762021-12-02T03:05:15ZPreparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release1178-2013https://doaj.org/article/e77f0be73c32467e81138cea0233d8762015-10-01T00:00:00Zhttps://www.dovepress.com/preparation-and-characterization-of-cefditoren-pivoxil-loaded-liposome-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Gojjala Venugopalarao,1 Rajasekhar Lakshmipathy,2 Nallani Chakravarthula Sarada1 1Environmental and Analytical Chemistry Division, School of Advanced Sciences, VIT University, Vellore, 2Centre for Material Science, KCG College of Technology, Chennai, India Background: The application of antibiotics has been limited due to weak biodistribution and pharmacokinetics. Encapsulation of these drugs in lipid vesicles might be a good solution for obtaining the required properties. Liposomes are one of the most suitable drug-delivery systems to deliver the drug to the target organ and minimize the distribution of the drug to non-target tissues.Objective: The study reported here aimed to develop cefditoren pivoxil liposomes by thin-film hydration, characterize them in terms of physical interactions, and undertake in vitro and in vivo release studies.Methodology: The pre-formulation studies were carried out using Fourier-transform infrared spectroscopy and differential scanning calorimetry. Cefditoren pivoxil liposomal formulations were formulated by thin-film hydration using biomaterials ie, soya lecithin and cholesterol in different molar ratios. The best molar ratio was determined by in vitro studies such as entrapment efficacy, particle size distribution, and diffusion.Results: From the in vitro release studies, it was found that the formulation that contained soya lecithin and cholesterol in a 1.0:0.6 molar ratio gave good entrapment of 72.33% and drug release of 92.5% at 36 hours. Further, the formulation’s zeta potential and surface morphology were examined and stability and in vivo studies were undertaken evaluating the pharmacokinetic parameters, which showed promising results.Conclusion: Formulation CPL VI showed the maximum drug-loading capacity of 72.3% with good controlled release and acceptable stability when compared with the other formulations. In vivo studies in rabbits showed that the drug release from the liposomes was successfully retarded with good controlled release behavior which can be used to treat many bacterial infections with a minimal dose. Keywords: biomaterials, liposomes, drug-delivery system, soya lecithin, cholesterolVenugopalarao GLakshmipathy RSarada NCDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss Supplement 1 Challenges in biomaterials research, Pp 149-157 (2015)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Venugopalarao G
Lakshmipathy R
Sarada NC
Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
description Gojjala Venugopalarao,1 Rajasekhar Lakshmipathy,2 Nallani Chakravarthula Sarada1 1Environmental and Analytical Chemistry Division, School of Advanced Sciences, VIT University, Vellore, 2Centre for Material Science, KCG College of Technology, Chennai, India Background: The application of antibiotics has been limited due to weak biodistribution and pharmacokinetics. Encapsulation of these drugs in lipid vesicles might be a good solution for obtaining the required properties. Liposomes are one of the most suitable drug-delivery systems to deliver the drug to the target organ and minimize the distribution of the drug to non-target tissues.Objective: The study reported here aimed to develop cefditoren pivoxil liposomes by thin-film hydration, characterize them in terms of physical interactions, and undertake in vitro and in vivo release studies.Methodology: The pre-formulation studies were carried out using Fourier-transform infrared spectroscopy and differential scanning calorimetry. Cefditoren pivoxil liposomal formulations were formulated by thin-film hydration using biomaterials ie, soya lecithin and cholesterol in different molar ratios. The best molar ratio was determined by in vitro studies such as entrapment efficacy, particle size distribution, and diffusion.Results: From the in vitro release studies, it was found that the formulation that contained soya lecithin and cholesterol in a 1.0:0.6 molar ratio gave good entrapment of 72.33% and drug release of 92.5% at 36 hours. Further, the formulation’s zeta potential and surface morphology were examined and stability and in vivo studies were undertaken evaluating the pharmacokinetic parameters, which showed promising results.Conclusion: Formulation CPL VI showed the maximum drug-loading capacity of 72.3% with good controlled release and acceptable stability when compared with the other formulations. In vivo studies in rabbits showed that the drug release from the liposomes was successfully retarded with good controlled release behavior which can be used to treat many bacterial infections with a minimal dose. Keywords: biomaterials, liposomes, drug-delivery system, soya lecithin, cholesterol
format article
author Venugopalarao G
Lakshmipathy R
Sarada NC
author_facet Venugopalarao G
Lakshmipathy R
Sarada NC
author_sort Venugopalarao G
title Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
title_short Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
title_full Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
title_fullStr Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
title_full_unstemmed Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
title_sort preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
publisher Dove Medical Press
publishDate 2015
url https://doaj.org/article/e77f0be73c32467e81138cea0233d876
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AT saradanc preparationandcharacterizationofcefditorenpivoxilloadedliposomesforcontrolledinvitroandinvivodrugrelease
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