Cargando…

Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles

Among the many methods available for solubility enhancement, mesoporous carriers are generating significant industrial interest. Owing to the spatial confinement of drug molecules within the mesopore network, low solubility crystalline drugs can be converted into their amorphous counterparts, which...

Descripción completa

Detalles Bibliográficos
Autores principales: Le, Tuan-Tu, Elzhry Elyafi, Abdul Khaliq, Mohammed, Afzal R., Al-Khattawi, Ali
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6630575/
https://www.ncbi.nlm.nih.gov/pubmed/31185610
http://dx.doi.org/10.3390/pharmaceutics11060269
_version_ 1783435334367838208
author Le, Tuan-Tu
Elzhry Elyafi, Abdul Khaliq
Mohammed, Afzal R.
Al-Khattawi, Ali
author_facet Le, Tuan-Tu
Elzhry Elyafi, Abdul Khaliq
Mohammed, Afzal R.
Al-Khattawi, Ali
author_sort Le, Tuan-Tu
collection PubMed
description Among the many methods available for solubility enhancement, mesoporous carriers are generating significant industrial interest. Owing to the spatial confinement of drug molecules within the mesopore network, low solubility crystalline drugs can be converted into their amorphous counterparts, which exhibit higher solubility. This work aims to understand the impact of drug overloading, i.e., above theoretical monolayer surface coverage, within mesoporous silica on the release behaviour and the thermal properties of loaded drugs. The study also looks at the inclusion of hypromellose acetate succinate (HPMCAS) to improve amorphisation. Various techniques including DSC, TGA, SEM, assay and dissolution were employed to investigate critical formulation factors of drug-loaded mesoporous silica prepared at drug loads of 100–300% of monolayer surface coverage, i.e., monolayer, double layer and triple layer coverage. A significant improvement in the dissolution of both Felodipine and Furosemide was obtained (96.4% and 96.2%, respectively). However, incomplete drug release was also observed at low drug load in both drugs, possibly due to a reversible adsorption to mesoporous silica. The addition of a polymeric precipitation inhibitor HPMCAS to mesoporous silica did not promote amorphisation. In fact, a partial coating of HPMCAS was observed on the exterior surface of mesoporous silica particles, which resulted in slower release for both drugs.
format Online
Article
Text
id pubmed-6630575
institution National Center for Biotechnology Information
language English
publishDate 2019
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-66305752019-08-19 Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles Le, Tuan-Tu Elzhry Elyafi, Abdul Khaliq Mohammed, Afzal R. Al-Khattawi, Ali Pharmaceutics Article Among the many methods available for solubility enhancement, mesoporous carriers are generating significant industrial interest. Owing to the spatial confinement of drug molecules within the mesopore network, low solubility crystalline drugs can be converted into their amorphous counterparts, which exhibit higher solubility. This work aims to understand the impact of drug overloading, i.e., above theoretical monolayer surface coverage, within mesoporous silica on the release behaviour and the thermal properties of loaded drugs. The study also looks at the inclusion of hypromellose acetate succinate (HPMCAS) to improve amorphisation. Various techniques including DSC, TGA, SEM, assay and dissolution were employed to investigate critical formulation factors of drug-loaded mesoporous silica prepared at drug loads of 100–300% of monolayer surface coverage, i.e., monolayer, double layer and triple layer coverage. A significant improvement in the dissolution of both Felodipine and Furosemide was obtained (96.4% and 96.2%, respectively). However, incomplete drug release was also observed at low drug load in both drugs, possibly due to a reversible adsorption to mesoporous silica. The addition of a polymeric precipitation inhibitor HPMCAS to mesoporous silica did not promote amorphisation. In fact, a partial coating of HPMCAS was observed on the exterior surface of mesoporous silica particles, which resulted in slower release for both drugs. MDPI 2019-06-10 /pmc/articles/PMC6630575/ /pubmed/31185610 http://dx.doi.org/10.3390/pharmaceutics11060269 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Le, Tuan-Tu
Elzhry Elyafi, Abdul Khaliq
Mohammed, Afzal R.
Al-Khattawi, Ali
Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles
title Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles
title_full Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles
title_fullStr Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles
title_full_unstemmed Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles
title_short Delivery of Poorly Soluble Drugs via Mesoporous Silica: Impact of Drug Overloading on Release and Thermal Profiles
title_sort delivery of poorly soluble drugs via mesoporous silica: impact of drug overloading on release and thermal profiles
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6630575/
https://www.ncbi.nlm.nih.gov/pubmed/31185610
http://dx.doi.org/10.3390/pharmaceutics11060269
work_keys_str_mv AT letuantu deliveryofpoorlysolubledrugsviamesoporoussilicaimpactofdrugoverloadingonreleaseandthermalprofiles
AT elzhryelyafiabdulkhaliq deliveryofpoorlysolubledrugsviamesoporoussilicaimpactofdrugoverloadingonreleaseandthermalprofiles
AT mohammedafzalr deliveryofpoorlysolubledrugsviamesoporoussilicaimpactofdrugoverloadingonreleaseandthermalprofiles
AT alkhattawiali deliveryofpoorlysolubledrugsviamesoporoussilicaimpactofdrugoverloadingonreleaseandthermalprofiles