Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats

Md Khalid Anwer,1 Muqtader Mohammad,1 Essam Ezzeldin,2,3 Farhat Fatima,1 Ahmed Alalaiwe,1 Muzaffar Iqbal2,3 1Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia; 2Department of Pharmaceutical Chemistry, College of Pharmacy, King Sau...

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Autores principales:	Anwer MK, Mohammad M, Ezzeldin E, Fatima F, Alalaiwe A, Iqbal M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Apremilast PLGA Nanoparticles Sustained release Pharmacokinetic profile Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/50123af8aa924a12a91645fb06c09f5c
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spelling	oai:doaj.org-article:50123af8aa924a12a91645fb06c09f5c2021-12-02T08:56:48ZPreparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats1178-2013https://doaj.org/article/50123af8aa924a12a91645fb06c09f5c2019-03-01T00:00:00Zhttps://www.dovepress.com/preparation-of-sustained-release-apremilast-loaded-plga-nanoparticles--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Md Khalid Anwer,1 Muqtader Mohammad,1 Essam Ezzeldin,2,3 Farhat Fatima,1 Ahmed Alalaiwe,1 Muzaffar Iqbal2,3 1Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia; 2Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 3Bioavailability Laboratory, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia Background: Apremilast (APM) is a novel, orally administered small molecule drug approved for treatment of psoriasis or psoriatic arthritis. Due to its low solubility and permeability, it is classified as a class IV drug according to BCS classification. Dose titration is recommended during APM treatment due to its tolerability and twice-daily dosing regimen issues. Materials and Methods: In this study, three different APM-loaded PLGA nanoparticles (F1–F3) were prepared by single emulsion and evaporation method. Based on particle size, PDI, zeta potential (ZP), entrapment efficiency (%EE), drug loading (%DL), and spectral characterization, the nanoparticles (F3) were optimized. The F3 nanoparticles were further evaluated for in vitro release and in vivo pharmacokinetic studies in rats. Results: The optimized nanoparticles (F3) had particles size 307.3±8.5 nm with a low PDI value 0.317, ZP of -43.4±2.6 mV, EE of 61.1±1.9% and DL of 1.9±0.1%. The in vitro release profile showed a sustained release pattern of F3 nanoparticles of APM. The pharmacokinetic results showed 2.25 times increase in bio-availability of F3 nanoparticles compared to normal APM suspension. Moreover, significant increase in half-life and mean residence time confirms long-term retention of F3 nanoparticles. Conclusion: Bioavailability enhancement along-with long-term retention of the APM-loaded PLGA nanoparticles might be helpful for the once-daily regimen treatment. Keywords: apremilast, Poly(D,L-lactide-coglycolide), nanoparticles, bioavailability, sustained releaseAnwer MKMohammad MEzzeldin EFatima FAlalaiwe AIqbal MDove Medical PressarticleApremilastPLGANanoparticlesSustained releasePharmacokinetic profileMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 1587-1595 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Apremilast PLGA Nanoparticles Sustained release Pharmacokinetic profile Medicine (General) R5-920
spellingShingle	Apremilast PLGA Nanoparticles Sustained release Pharmacokinetic profile Medicine (General) R5-920 Anwer MK Mohammad M Ezzeldin E Fatima F Alalaiwe A Iqbal M Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
description	Md Khalid Anwer,1 Muqtader Mohammad,1 Essam Ezzeldin,2,3 Farhat Fatima,1 Ahmed Alalaiwe,1 Muzaffar Iqbal2,3 1Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia; 2Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 3Bioavailability Laboratory, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia Background: Apremilast (APM) is a novel, orally administered small molecule drug approved for treatment of psoriasis or psoriatic arthritis. Due to its low solubility and permeability, it is classified as a class IV drug according to BCS classification. Dose titration is recommended during APM treatment due to its tolerability and twice-daily dosing regimen issues. Materials and Methods: In this study, three different APM-loaded PLGA nanoparticles (F1–F3) were prepared by single emulsion and evaporation method. Based on particle size, PDI, zeta potential (ZP), entrapment efficiency (%EE), drug loading (%DL), and spectral characterization, the nanoparticles (F3) were optimized. The F3 nanoparticles were further evaluated for in vitro release and in vivo pharmacokinetic studies in rats. Results: The optimized nanoparticles (F3) had particles size 307.3±8.5 nm with a low PDI value 0.317, ZP of -43.4±2.6 mV, EE of 61.1±1.9% and DL of 1.9±0.1%. The in vitro release profile showed a sustained release pattern of F3 nanoparticles of APM. The pharmacokinetic results showed 2.25 times increase in bio-availability of F3 nanoparticles compared to normal APM suspension. Moreover, significant increase in half-life and mean residence time confirms long-term retention of F3 nanoparticles. Conclusion: Bioavailability enhancement along-with long-term retention of the APM-loaded PLGA nanoparticles might be helpful for the once-daily regimen treatment. Keywords: apremilast, Poly(D,L-lactide-coglycolide), nanoparticles, bioavailability, sustained release
format	article
author	Anwer MK Mohammad M Ezzeldin E Fatima F Alalaiwe A Iqbal M
author_facet	Anwer MK Mohammad M Ezzeldin E Fatima F Alalaiwe A Iqbal M
author_sort	Anwer MK
title	Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
title_short	Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
title_full	Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
title_fullStr	Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
title_full_unstemmed	Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
title_sort	preparation of sustained release apremilast-loaded plga nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/50123af8aa924a12a91645fb06c09f5c
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_version_	1718398301007511552

Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats

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