A Novel Oral Drugs Delivery System for Borneol Based on HiCap®100 and Maltodextrin: Preparation, Characterization, and the Investigation as an Intestinal Absorption Enhancer.

Abstract

The objective of this study was to create a new method for delivering oral borneol (BN) drug that would improve stability. This was accomplished through microencapsulation using HiCap®100 and maltodextrin (MD), resulting in HiCap®100/MD/BN microcapsules (MCs). The HiCap®100/MD/BN MCs were evaluated in terms of encapsulation efficiency (EE%), drug loading (DL%), morphological observations, particle size distribution, Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), thermal analysis, drug degradation rate studies, and in vitro release behavior. The effect of MCs on intestinal permeability in a rat model was assessed using the model drug "florfenicol" (FF) in single-pass intestinal perfusion (SPIP) study. The relationship between MCs and P-glycoprotein (P-gp) was further investigated in comparison with verapamil (Ver). The irritation of MCs was assessed by histological analysis. The MCs in a spherical structure with micron-scale dimensions were obtained. The EE% and DL% were (86.71 ± 0.96)% and (6.03 ± 0.32)%, respectively. MCs played a significantly protective role in drug degradation rate studies. In vitro release studies indicated that the release behavior of MCs was significantly better than BN at the three-release media, and the cumulative release rate exceeded 90% in 15 min. The SPIP studies showed that MCs significantly enhanced the absorption of FF in rats. Compared with Ver, MCs were not promoted by a single inhibition of P-gp. Hematoxylin-eosin (HE)-stained images showed that MCs had no obvious irritation and toxic effects on the intestines of rats. Thus, the preparation of HiCap®100/MD/BN MCs improves the stability of BN, which has certain scientific value for the development and application of BN, and provides unique perspectives for future BN-related researches.