Preparation and In Vitro and In Vivo Evaluation of Rectal In Situ Gel of Meloxicam Hydroxypropyl-β-cyclodextrin Inclusion Complex

Authors:
Open Access
Publisher website
Google Scholar
Abstract
Meloxicam (MLX) is one of the most effective NSAIDs, but its poor water solubility and low bioavailability limit its clinical application. In this study, we designed a thermosensitive in situ gel of the hydroxypropyl-β-cyclodextrin inclusion complex (MLX/HP-β-CD-ISG) for rectal delivery to improve bioavailability. The best method for preparing MLX/HP-β-CD was the saturated aqueous solution method. The optimal inclusion prescription was optimized using an orthogonal test, and the inclusion complex was evaluated via PXRD, SEM, FTIR and DSC. Then, MLX/HP-β-CD-ISG was characterized regarding the gel properties, release in vitro, and pharmacokinetics in vivo. The inclusion rate of the inclusion complex obtained via the optimal preparation process was 90.32 ± 3.81%. The above four detection methods show that MLX is completely embedded in the HP-β-CD cavity. The developed MLX/HP-β-CD-ISG formulation has a suitable gelation temperature of 33.40 ± 0.17 °C, a gelation time of 57.33 ± 5.13 s, pH of 7.12 ± 0.05, good gelling ability and meets the requirements of rectal preparations. More importantly, MLX/HP-β-CD-ISG significantly improved the absorption and bioavailability of MLX in rats, prolonging the rectal residence time without causing rectal irritation. This study suggests that the MLX/HP-β-CD-ISG can have a wide application prospect with superior therapeutic benefits.
Funding Information
  • National Natural Science Foundation of China (81960720, 82260771, 20224BAB206117, CXTD22001, 2022BSZR004)
  • The Project of Natural Science Foundation of Jiangxi Province (81960720, 82260771, 20224BAB206117, CXTD22001, 2022BSZR004)
  • Jiangxi University of Chinese Medicine Science and Technology Innovation Team Development Program (81960720, 82260771, 20224BAB206117, CXTD22001, 2022BSZR004)
  • Jiangxi University of Chinese Medicine Doctoral Research Start-up Fund Project (81960720, 82260771, 20224BAB206117, CXTD22001, 2022BSZR004)
  • Long-term Project of Innovative Leading Talents of Jiangxi “Double Thousand Plan” (81960720, 82260771, 20224BAB206117, CXTD22001, 2022BSZR004)

This publication has 37 references indexed in Scilit: