Orally Deliverable Dual-Targeted Pellets for the Synergistic Treatment of Ulcerative Colitis

Xiaomeng Tang,1– 3,* Meng Yang,4,* Yongwei Gu,1,2 Liangdi Jiang,1,2,5 Yue Du,1,2,5 Jiyong Liu1– 3 1Department of Pharmacy, Fudan University Shanghai Cancer Center, Fudan University, Shanghai, 200032, People’s Republic of China; 2Department of Oncology, Shanghai Medical College, Fudan University, Shanghai, 200032, People’s Republic of China; 3Department of Pharmacy, Changhai Hospital, Naval Medical University, Shanghai, 200433, People’s Republic of China; 4Department of Pharmacy, Shanghai Ninth People Hospital, Shanghai Jiao Tong University, Shanghai, 200011, People’s Republic of China; 5College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, Shandong, 250355, People’s Republic of China*These authors contributed equally to this workCorrespondence: Jiyong LiuDepartment of Pharmacy, Fudan University Shanghai Cancer Center, Fudan University, Shanghai, 200032, People’s Republic of ChinaTel/Fax +86-21-64175590Email liujiyong@fudan.edu.cnPurpose: The effective treatment of ulcerative colitis (UC) poses substantial challenges, and the aetiopathogenesis of UC is closely related to infectious, immunological and environmental factors. Currently, there is a considerable need for the development of orally bioavailable dosage forms that enable the effective delivery of therapeutic drugs to local diseased lesions in the gastrointestinal tract.Methods: Berberine (BBR) and Atractylodes macrocephala Koidz (AM) volatile oil, derived from the Chinese herbs Coptis chinensis Franch and Atractylodes macrocephala Koidz, have anti-inflammatory and immunomodulatory activities. In this study, we prepared colon-targeted pellets loaded with BBR and stomach-targeted pellets loaded with AM volatile oil for the synergistic treatment of UC. The Box–Behnken design and β-cyclodextrin inclusion technique were used to optimize the enteric coating formula and prepare volatile oil inclusion compounds.Results: The two types of pellets were spherical and had satisfactory physical properties. The ...