S A Sreenivas1 ,
K V Pai2
1Department of Pharmaceutics, KLES's College of Pharmacy, Vidyanagar, Hubli, Karnataka.;
2Department of Industrial Chemistry, Shankaraghatta, Shimoga, Karnataka, India..
For correspondence:- S Sreenivas
Email: saiseenu7@rediffmail.com Tel:09242892034
Published: 20 September 2008
Citation:
Sreenivas SA, Pai KV.
Thiolated Chitosans: Novel Polymers for Mucoadhesive Drug Delivery - A Review. Trop J Pharm Res 2008; 7(3):1077-1088
doi:
10.4314/tjpr.v7i3.10
© 2008 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
Abstract
Chitosan is a natural polycationic copolymer consisting of glucosamine and N-acetylglucosamine units. The polymer has valuable properties as a biomaterial because it is considered to be biocompatible, biodegradable and non-toxic. The purpose of this review article is to provide detailed information about thiolated chitosans which are gaining popularity because of their high mucoadhsiveness and extended drug release properties. The derivatization of the primary amino groups of chitosan with coupling reagents bearing thiol functions leads to the formation of thiolated chitosans. Various properties of chitosan are improved by the immobilization of thiol groups. Due to the formation of disulfide bonds with mucus glycoproteins, mucoadhesiveness is augmented. The permeation of paracellular markers through mucosa can be enhanced by utilizing thiolated instead of unmodified chitosan. Moreover, thiolated chitosans display in situ gelling features due to the pH-dependent formation of inter- as well as intra-molecular disulfide bonds. This latter process provides, strong cohesion and stability of carrier matrices, being based on thiolated chitosans. The in situ gel formation within the pH range of 5 to 6.8 makes the application of thiolated chitosans on vaginal, nasal and ocular mucosa also possible. Thiolated chitosans can guarantee prolonged controlled release of embedded therapeutic ingredients.
Keywords: Thiolated chitosan,Thiomers, Mucoadhesion, Permeation enhancement, In situ gelation