Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.

Controlled-release microparticles offer a promising avenue for enhancing patient compliance and minimizing dosage frequency. In this study, we aimed to design controlled-release microparticles of Glipizide utilizing Eudragit S100 and Methocel K 100 M polymers as controlling agents. The microparticle...

Full description

Saved in:
Bibliographic Details
Main Authors: Qaiser Rasheed, Kamran Ahmad Khan, Ghulam Razaque, Ashfaq Ahmad, Asif Nawaz, Naheed Akhtar, Kifayat Ullah Shah, Zahid Rasul Niazi, Muhammad Danish Saeed, Anila Alam
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2025-01-01
Series:PLoS ONE
Online Access:https://doi.org/10.1371/journal.pone.0313523
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1841533158776897536
author Qaiser Rasheed
Kamran Ahmad Khan
Ghulam Razaque
Ashfaq Ahmad
Asif Nawaz
Naheed Akhtar
Kifayat Ullah Shah
Zahid Rasul Niazi
Muhammad Danish Saeed
Anila Alam
author_facet Qaiser Rasheed
Kamran Ahmad Khan
Ghulam Razaque
Ashfaq Ahmad
Asif Nawaz
Naheed Akhtar
Kifayat Ullah Shah
Zahid Rasul Niazi
Muhammad Danish Saeed
Anila Alam
author_sort Qaiser Rasheed
collection DOAJ
description Controlled-release microparticles offer a promising avenue for enhancing patient compliance and minimizing dosage frequency. In this study, we aimed to design controlled-release microparticles of Glipizide utilizing Eudragit S100 and Methocel K 100 M polymers as controlling agents. The microparticles were fabricated through a simple solvent evaporation method, employing various drug-to-polymer ratios to formulate different controlled-release batches labeled as F1 to F5. Evaluation of the microparticles encompassed a range of parameters including flow properties, particle size, morphology, percentage yield, entrapment efficiencies, percent drug loading, and dissolution studies. Additionally, various kinetic models were employed to elucidate the drug release mechanism. Furthermore, difference and similarity factors were utilized to compare the dissolution profiles of the tested formulations with a reference formulation. The compressibility index and angle of repose indicated favorable flow properties of the prepared microparticles, with values falling within the range of 8 to 10 and 25 to 29, respectively. The particle size distribution of the microparticles ranged from 95.3 to 126 μm. Encouragingly, the microparticles exhibited high percent yield (ranging from 66 to 77%), entrapment efficiency (80 to 96%), and percent drug loading (46 to 54%). All formulated batches demonstrated controlled drug release profiles extending up to 12 hours, with glipizide release following an anomalous non-Fickian diffusion pattern. However, the drug release profiles of the reference formulation and various polymeric microparticles did not meet the acceptable limits of difference and similarity factors. In-vivo studies revealed sustained hypoglycemic effects over a 12-hour period, indicating the efficacy of the controlled-release microparticles. Overall, our findings suggest the successful utilization of polymeric materials in designing controlled-release microparticles, thereby reducing dosage frequency and potentially improving patient compliance.
format Article
id doaj-art-5b7ebef8bc214e70ae60b1c638d746b5
institution Kabale University
issn 1932-6203
language English
publishDate 2025-01-01
publisher Public Library of Science (PLoS)
record_format Article
series PLoS ONE
spelling doaj-art-5b7ebef8bc214e70ae60b1c638d746b52025-01-17T05:31:29ZengPublic Library of Science (PLoS)PLoS ONE1932-62032025-01-01201e031352310.1371/journal.pone.0313523Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.Qaiser RasheedKamran Ahmad KhanGhulam RazaqueAshfaq AhmadAsif NawazNaheed AkhtarKifayat Ullah ShahZahid Rasul NiaziMuhammad Danish SaeedAnila AlamControlled-release microparticles offer a promising avenue for enhancing patient compliance and minimizing dosage frequency. In this study, we aimed to design controlled-release microparticles of Glipizide utilizing Eudragit S100 and Methocel K 100 M polymers as controlling agents. The microparticles were fabricated through a simple solvent evaporation method, employing various drug-to-polymer ratios to formulate different controlled-release batches labeled as F1 to F5. Evaluation of the microparticles encompassed a range of parameters including flow properties, particle size, morphology, percentage yield, entrapment efficiencies, percent drug loading, and dissolution studies. Additionally, various kinetic models were employed to elucidate the drug release mechanism. Furthermore, difference and similarity factors were utilized to compare the dissolution profiles of the tested formulations with a reference formulation. The compressibility index and angle of repose indicated favorable flow properties of the prepared microparticles, with values falling within the range of 8 to 10 and 25 to 29, respectively. The particle size distribution of the microparticles ranged from 95.3 to 126 μm. Encouragingly, the microparticles exhibited high percent yield (ranging from 66 to 77%), entrapment efficiency (80 to 96%), and percent drug loading (46 to 54%). All formulated batches demonstrated controlled drug release profiles extending up to 12 hours, with glipizide release following an anomalous non-Fickian diffusion pattern. However, the drug release profiles of the reference formulation and various polymeric microparticles did not meet the acceptable limits of difference and similarity factors. In-vivo studies revealed sustained hypoglycemic effects over a 12-hour period, indicating the efficacy of the controlled-release microparticles. Overall, our findings suggest the successful utilization of polymeric materials in designing controlled-release microparticles, thereby reducing dosage frequency and potentially improving patient compliance.https://doi.org/10.1371/journal.pone.0313523
spellingShingle Qaiser Rasheed
Kamran Ahmad Khan
Ghulam Razaque
Ashfaq Ahmad
Asif Nawaz
Naheed Akhtar
Kifayat Ullah Shah
Zahid Rasul Niazi
Muhammad Danish Saeed
Anila Alam
Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.
PLoS ONE
title Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.
title_full Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.
title_fullStr Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.
title_full_unstemmed Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.
title_short Fabrication of glipizide loaded polymeric microparticles; in-vitro and in-vivo evaluation.
title_sort fabrication of glipizide loaded polymeric microparticles in vitro and in vivo evaluation
url https://doi.org/10.1371/journal.pone.0313523
work_keys_str_mv AT qaiserrasheed fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT kamranahmadkhan fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT ghulamrazaque fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT ashfaqahmad fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT asifnawaz fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT naheedakhtar fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT kifayatullahshah fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT zahidrasulniazi fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT muhammaddanishsaeed fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation
AT anilaalam fabricationofglipizideloadedpolymericmicroparticlesinvitroandinvivoevaluation