Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Formulation and Evaluation of Bupivacaine-Loaded Glutaraldehyde-Crosslinked High Molecular Weight Chitosan Microspheres

Murugesh Shivashankar¹, Badal Kumar Mandal²

¹Pharmaceutical Chemistry Division; ²Environmental and Analytical Chemistry Division, School of Advanced Sciences, VIT University, Vellore 632014, Tamilnadu, India.

For correspondence:- Badal Mandal Email: badalmandal@vit.ac.in Tel:+9104162202339

Received: 22 November 2012 Accepted: 15 January 2012 Published: 21 February 2013

Citation: Shivashankar M, Mandal BK. Formulation and Evaluation of Bupivacaine-Loaded Glutaraldehyde-Crosslinked High Molecular Weight Chitosan Microspheres. Trop J Pharm Res 2013; 12(1):13-18 doi: 10.4314/tjpr.v12i1.3

© 2013 The authors.
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Abstract

Purpose: To develop a chitosan microsphere carrier system of bupivacaine for buccal administration.

Methods: Chitosan microspheres loaded with bupivacaine were prepared by emulsification technique based on glutaraldehyde cross-linking and drug-loaded chitosan microsphere were coated with poly-glycolic acid (PGA) film The formulated microspheres were characterized by x-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and in vitro release was performed in pH 7.4 phosphate buffer both in the presence and in absence of lysozyme.

Results: Encapsulation yield was 83.1 %. SEM studies indicate that the microspheres were spherical and had a relatively smooth surface. XRD and DSC data indicate that there was no interaction between the drug and polymer. In vitro results show that in the presence of lysozyme, 39 % of the drug was released from the microspheres after 4.5 days while maximum drug release (42.5 %) was achieved on day 11. This compares with 31 % drug release on 4.5^th day and 38 % on 11^th day; maximum drug release occurred on day 11 in the absence of lysozyme.

Conclusion: It is evident from this study that microspheres can potentially be used for controlled release of of bupivacaine for the management of dental pain in the buccal cavity.

Keywords: Cross-linked chitosan, Microsphere, In vitro release, Oral drug delivery, Bupivacaine, Local anesthesia