title: Nanoencapsulation of psoralidin via chitosan and Eudragit S100 for enhancement of oral bioavailability.
abstract: Psoralidin (PL) has recently been attracting more attention as a new anticancer agent candidate. Nevertheless, peroral administration of PL is largely challenged by its insoluble nature and intestinal efflux. This article aimed to develop a nanoencapsulation formulation of PL using water-soluble chitosan and Eudragit S100 and to evaluate its potential for bioavailability enhancement. PL-loaded nanocapsules (PL-NCs) were prepared by a solvent diffusion and high-pressure homogenization technique with Poloxamer 188 as a stabilizer. The resultant PL-NCs were approximately 132.5nm in particle size and possessed a high entrapment efficiency (98.1%). In vitro release showed that PL was released less from the nanocapsules due to electrostatic complexation. A lipolytic experiment demonstrated that our prepared PL-NCs were not degraded by lipase, in contrast with the most commonly used lipid nanoparticles. Furthermore, PL-NCs appeared to have less affinity for intestinal mucins. Following oral administration, the bioavailability of PL was significantly enhanced via the PL-NCs, with a value of 339.02% relative to the reference (suspensions). Excellent intestinal adhesion and transepithelial permeability accounted for the enhancement of oral bioavailability. Taken together, these results indicate that nanoencapsulation of PL with chitosan and Eudragit S100 is a promising strategy for improved PL oral delivery.
authors.affiliation: Department of Pharmaceutics, Huaihe Hospital Affiliated with Henan University, No. 1 Baobei Road, Kaifeng 475000, PR China.
authors.forename: Juntao
authors.initials: J
authors.lastname: Yin
authors.affiliation: Department of Pharmaceutics, Huaihe Hospital Affiliated with Henan University, No. 1 Baobei Road, Kaifeng 475000, PR China.
authors.forename: Cuiyu
authors.initials: C
authors.lastname: Xiang
authors.affiliation: Department of Pharmaceutics, Huaihe Hospital Affiliated with Henan University, No. 1 Baobei Road, Kaifeng 475000, PR China. Electronic address: sxyyjk@sina.com.
authors.forename: Xiaoyong
authors.initials: X
authors.lastname: Song
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001572:Benzofurans / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D003374:Coumarins / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D001572:Benzofurans; D003374:Coumarins; D053769:Nanocapsules; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D048271:Chitosan; C102768:psoralidin
keywords: Bioavailability; Chitosan; Eudragit S100; Nanoencapsulation; Permeability; Psoralidin