Preparation and in vitro release kinetics of ivermectin sustained-release bolus optimized by response surface methodology.

Abstract

Sustained-release formulations of ivermectin (IVM) are useful for controlling parasitic diseases in animals. In this work, an IVM bolus made from microcrystalline cellulose (MCC), starch and low-substituted hydroxypropyl cellulose (LS-HPC) was optimized by response surface methodology. The bolus was dissolved in a cup containing 900 mL of dissolution medium at 39.5 °C, under with stirring at 100 rpm. A quadratic model was formulated using analysis of variance according to the dissolution time. The optimized formulation of the bolus contained 8% MCC, 0.5% starch, and 0.25% LS-HPC. The length, width, and height of the prepared IVM bolus were 28.12 ± 0.14, 16.1 ± 0.13, and 13.03 ± 0.05 mm, respectively. The bolus weighed 11.4842 ± 0.1675 g (with a density of 1.95 g/cm3) and contained 458.26 ± 6.68 mg of IVM. It exhibited in vitro sustained-release for over 60 days, with a cumulative amount and percentage of released IVM of 423.72 ± 5.48 mg and 92.52 ± 1.20%, respectively. The Korsmeyer-Peppas model provided the best fit to the dissolution release kinetics, exhibiting an R2 value close to 1 and the lowest Akaike Information Criterion among different models. The parameter n (0.5180) of the Korsmeyer-Peppas model was between 0.45 and 0.89. It was demonstrated that the release mechanism of the IVM bolus followed a diffusive erosion style.

• Authors: Xiangchun Ruan, Xiuge Gao, Ying Gao, Lin Peng, Hui Ji, Dawei Guo, Shanxiang Jiang
• Journal: PeerJ (PeerJ) Vol. 6 Pg. e5418 ( 2018) ISSN: 2167-8359 [Print] United States
• PMID: 30083480 (Publication Type: Journal Article)