Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery

INTRODUCTION: The complexity of the brain is a crucial ratelimiting factor in developing new drugs for the central nervous system (CNS). The blood–brain barrier and the blood–cerebrospinal fluid barrier play major role in restricting systemic drug delivery to the CNS. The unique neuronal connection...

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Main Authors:	Mohananaidu, Keithanchali, Chatterjee, Bappaditya
Format:	Conference or Workshop Item
Language:	English English English
Published:	2018
Subjects:	RS192 Materia Medica-Pharmaceutical Technology
Online Access:	http://irep.iium.edu.my/68355/ http://irep.iium.edu.my/68355/1/PRCO08%20%28Anjali%29.pdf http://irep.iium.edu.my/68355/7/4IPRC.pdf http://irep.iium.edu.my/68355/12/IPRC%20Presentation%20Anjali.pdf

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spelling	iium-683552018-12-27T07:41:59Z http://irep.iium.edu.my/68355/ Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery Mohananaidu, Keithanchali Chatterjee, Bappaditya RS192 Materia Medica-Pharmaceutical Technology INTRODUCTION: The complexity of the brain is a crucial ratelimiting factor in developing new drugs for the central nervous system (CNS). The blood–brain barrier and the blood–cerebrospinal fluid barrier play major role in restricting systemic drug delivery to the CNS. The unique neuronal connection of the nose and CNS, has given rise to intranasal drug delivery to brain bypassing the barriers. OBJECTIVES: This research aims to fabricate a thermoresponsive in situ gel drug delivery system for pregabalin, a neuropathic drug, via naso-mucosal route targeting brain. METHODS: A thermoresponsive in situ gel was developed by mixing 15-20% Poloxamer 407 with 0.15-0.25% Carrageenan to 1% pregabalin solution (weight ratio) by cold method. The formulations became liquid when stored at 2-8 ̊ C. The gelation temperature and pH for the in situ gels were 35-37 ̊ C and 6.0-6.5 respectively. Rheology study of the gel by a Haake-Mars programmable rheometer showed pseudoplasticity and distinct shear-thinning with increasing shear stress. CT3 Texture analyzer was used to determine the mucoadhesion strength of the gel using goat nasal mucosa. Ex-vivo drug permeation study through goat nasal mucosa was done using Franz diffusion cell. Pregabalin was quantified in formulation and ex-vivo permeated samples by a developed ATR-FTiR method. RESULTS: It was shown that only poloxamer containing gel had lesser mucoadhesion strength compared to that containing poloxamer-carrageenan both. Permeation flux was shown to be greater in case of thermoreversible gel compared to normal solution. This is because of higher retention of formulation on nasal mucosa. CONCLUSION: From in-vitro studies, it can be concluded that the in situ gelling system can result in higher nasal epithelial permeation, which could deliver drug to the brain efficiently. The brain distribution study of the drug using the developed in-situ gel is subjected to future in-vivo study in animal model. 2018-08 Conference or Workshop Item NonPeerReviewed application/pdf en http://irep.iium.edu.my/68355/1/PRCO08%20%28Anjali%29.pdf application/pdf en http://irep.iium.edu.my/68355/7/4IPRC.pdf application/pdf en http://irep.iium.edu.my/68355/12/IPRC%20Presentation%20Anjali.pdf Mohananaidu, Keithanchali and Chatterjee, Bappaditya (2018) Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery. In: 4th International Pharmaceutical Research Conference 2018, 25th-26th August 2018, Cyberjaya, Malaysia. (Unpublished)
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
language	English English English
topic	RS192 Materia Medica-Pharmaceutical Technology
spellingShingle	RS192 Materia Medica-Pharmaceutical Technology Mohananaidu, Keithanchali Chatterjee, Bappaditya Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery
description	INTRODUCTION: The complexity of the brain is a crucial ratelimiting factor in developing new drugs for the central nervous system (CNS). The blood–brain barrier and the blood–cerebrospinal fluid barrier play major role in restricting systemic drug delivery to the CNS. The unique neuronal connection of the nose and CNS, has given rise to intranasal drug delivery to brain bypassing the barriers. OBJECTIVES: This research aims to fabricate a thermoresponsive in situ gel drug delivery system for pregabalin, a neuropathic drug, via naso-mucosal route targeting brain. METHODS: A thermoresponsive in situ gel was developed by mixing 15-20% Poloxamer 407 with 0.15-0.25% Carrageenan to 1% pregabalin solution (weight ratio) by cold method. The formulations became liquid when stored at 2-8 ̊ C. The gelation temperature and pH for the in situ gels were 35-37 ̊ C and 6.0-6.5 respectively. Rheology study of the gel by a Haake-Mars programmable rheometer showed pseudoplasticity and distinct shear-thinning with increasing shear stress. CT3 Texture analyzer was used to determine the mucoadhesion strength of the gel using goat nasal mucosa. Ex-vivo drug permeation study through goat nasal mucosa was done using Franz diffusion cell. Pregabalin was quantified in formulation and ex-vivo permeated samples by a developed ATR-FTiR method. RESULTS: It was shown that only poloxamer containing gel had lesser mucoadhesion strength compared to that containing poloxamer-carrageenan both. Permeation flux was shown to be greater in case of thermoreversible gel compared to normal solution. This is because of higher retention of formulation on nasal mucosa. CONCLUSION: From in-vitro studies, it can be concluded that the in situ gelling system can result in higher nasal epithelial permeation, which could deliver drug to the brain efficiently. The brain distribution study of the drug using the developed in-situ gel is subjected to future in-vivo study in animal model.
format	Conference or Workshop Item
author	Mohananaidu, Keithanchali Chatterjee, Bappaditya
author_facet	Mohananaidu, Keithanchali Chatterjee, Bappaditya
author_sort	Mohananaidu, Keithanchali
title	Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery
title_short	Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery
title_full	Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery
title_fullStr	Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery
title_full_unstemmed	Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery
title_sort	development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery
publishDate	2018
url	http://irep.iium.edu.my/68355/ http://irep.iium.edu.my/68355/1/PRCO08%20%28Anjali%29.pdf http://irep.iium.edu.my/68355/7/4IPRC.pdf http://irep.iium.edu.my/68355/12/IPRC%20Presentation%20Anjali.pdf
first_indexed	2023-09-18T21:37:01Z
last_indexed	2023-09-18T21:37:01Z
_version_	1777412888275714048

Development and characterization of a thermoreversible gel formulation of pregabalin for intranasal delivery

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