FORMULATION AND EVALUATION OF TINIDAZOLE-LOADED ALGINATE MICRO-BEADS FOR COLON DELIVERY

FORMULATION AND EVALUATION OF TINIDAZOLE-LOADED ALGINATE MICRO-BEADS FOR COLON DELIVERY

CHEKWUBE ANDREW EZEGBE1,* , OLUEBUBE CHISOM ONYIA1 , PECULIAR FENNA

ONYEKERE2 , AMARACHI GRACE EZEGBE3 , AMARACHI AGU KALU1 , UGOCHI ELIZABETH

IKE-ONYISHI2

 

  1. Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka. 410001. Enugu State, Nigeria.
  1. Department of Pharmacognosy and Environmental Medicine, University of Nigeria, Nsukka. 410001. Enugu State, Nigeria.
  1. Department of Home Science and Management, University of Nigeria, Nsukka. 410001. Enugu State, Nigeria.

Afr. J Pharm Res Dev; Volume 13(1): 076-086 (2021)

ABSTRACT

The colon is a site that allows for both systemic and local delivery of drugs. Colon-targeted drugs are more effective therapeutically with reduced systemic effects. In this study, we developed tinidazole microbeads using a combination of lipids, surfactants and synthetic polymers to produce extended release formulation of tinidazole beads and to minimize the systemic side effects. Tinidazole loaded microbeads were formulated using emulsification ionic gelation technique. The resulting beads were coated differently with Eudragits and Kollicoat. They were evaluated for drug content, encapsulation efficiency, particle size and morphology, thermal analysis, in vitro in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.2) and in vivo release properties. The encapsulation efficiency range was within 47 ± 0.08 to 93.6 ± 0.02 % and the particle size was within 32.7 ± 0.08 to 44.4 ± 0.09 µm. Batch T4 was the best batch of the formulations as it gave the highest EE and in vitro release. The swelling index result obtained, showed that batch T1 did not swell in pH 1.2, while batches T2-T4 showed swelling ability. The in vivo studies showed that after 24 h, the uncoated batch T4 achieved peak serum concentration of 293.37 µg/ml, while the marketed sample achieved peak serum concentration of 188.21 µg/ml at 24 h. The characterization studies showed that the alginate beads could be considered as potential systems for colon delivery of tinidazole for use in the treatment of amoebic infection.

Email of correspondence: ezegbe.chekwube@unn.edu.ng

KEYWORDS: Alginate beads; Colon delivery; Tinidazole; Kollicoat®; Eudragits®.