Micro- and Nanoencapsulated Hybrid Delivery System (MNEHDS): A Novel Approach for Colon-Targeted Oral Delivery of Berberine

• DOI: 10.1021/acs.molpharmaceut.0c00970
• Publication Date: 2021-02-25T16:00:52Z
• Authors: Lingzhi Zhang; Mingyan Li; Guiqiu Zhang; Changxing Gao; Shengfang Wang; Tingting Zhang; Chen Ma; Lianyan Wang; Qing Zhu
• Keywords: 0303 health sciences; Berberine; Colon; Dextran Sulfate; Administration, Oral; Colitis; 3. Good health; Disease Models, Animal; Drug Liberation; Mice; 03 medical and health sciences; Drug Delivery Systems; Polylactic Acid-Polyglycolic Acid Copolymer; Polymethacrylic Acids; Delayed-Action Preparations; Animals; Humans; Nanoparticles; Female; Intestinal Mucosa; Particle Size

Berberine (BBR) is currently explored in the oral treatment of many disorders, especially those involving inflammatory processes. Nanotechnology-based drug delivery systems are emerging as an effective approach for improving poor absorption/bioavailability BBR. To optimize BBR immunoregulatory effects on a specific part gastrointestinal tract, here we describe micro- and nanoencapsulated hybrid system (MNEHDS) colon-targeted test its therapeutic efficacy murine colitis model. The MNEHDS formed by encapsulation BBR-loaded poly(lactic-co-glycolic acid) nanoparticles into pH-sensitive, BBR-pre-entrapped Eudragit FS30D matrix to form microparticle composed nanoparticles. Once colonic environment, microencapsulated almost completely released immediate action, while can provide sustained release subsequent their intestinal absorption. One dose MNEHDS/BBR results significant attenuation acute induced dextran sulfate sodium. also proves be during chronically with two doses given 1 week apart. improved accompanied decreased production colon inflammation. Comparatively, one or 7-day courses free has less effect ameliorating either chronic colitis. Thus, represents novel BBR, potentially other agents, treat bowel disease.