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

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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.

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Data is available from the corresponding author upon request.

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Funding

This work was financially supported by the Guangzhou Science and Technology Plan Project (number 201904010112) and the “Yang Fan Plan” team project of Guangdong Province (No. 2017YT05S137).

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmacy, Guangzhou Higher Education Mega Center, Guangdong Pharmaceutical University, 280 East Waihuan Road, Guangzhou, 510006, China

    Yuan Chen, Xiaowei Jin & Bohong Guo

  2. Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System, Guangdong Pharmaceutical University, Guangzhou, 510006, People’s Republic of China

    Yuan Chen, Xiaowei Jin & Bohong Guo

  3. Guangdong Baiyun Mountain and Hutchison Whampoa Ltd., Modern Chinese Medicine Research Institute, Guangzhou, 510515, China

    Yanhui Kuang, Sisi Zhang, Chuanping Zhang & Chuyuan Li

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  1. Yuan Chen
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  3. Yanhui Kuang
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Contributions

YC: conceptualization, investigation, methodology, formal analysis, data curation, writing — original draft. XJ: conceptualization, methodology, investigation, writing — review and editing. YK: investigation, validation. SZ: resources, project administration. CZ: literature search, data acquisition. CL: data acquisition. BG: project administration, supervision, writing — original draft, writing — review and editing, funding acquisition.

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Correspondence to Bohong Guo.

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Chen, Y., Jin, X., Kuang, Y. et al. A Novel Oral Drugs Delivery System for Borneol Based on HiCap®100 and Maltodextrin: Preparation, Characterization, and the Investigation as an Intestinal Absorption Enhancer. AAPS PharmSciTech 24, 197 (2023). https://doi.org/10.1208/s12249-023-02654-0

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