title: Improved oral bioavailability of capsaicin via liposomal nanoformulation: preparation, in vitro drug release and pharmacokinetics in rats.
abstract: This study innovatively prepared an effective capsaicin-loaded liposome, a nanoformulation with fewer irritants, for oral administration. The in vitro and in vivo properties of the liposomal encapsulation were investigated and the potential possibility of oral administration evaluated. The liposomal agent composed of phospholipid, cholesterol, sodium cholate and isopropyl myristate was prepared using film-dispersion method. A level A in vitro-in vivo correlation (IVIVC) was established for the first time, which demonstrated an excellent IVIVC of both formulated and free capsaicin in oral administration. Physicochemical characterizations including mean particle size, zeta (ζ) potential and average encapsulation efficiency of capsaicin-loaded liposome were found to be 52.2 ± 1.3 nm, -41.5 ± 2.71 mv and 81.9 ± 2.43 %, respectively. In vivo, liposomal encapsulation allowed a 3.34-fold increase in relative bioavailability compared to free capsaicin. The gastric mucosa irritation studies indicated that the liposomal system was a safe carrier for oral administration. These results support the fact that capsaicin, an effective drug for the treatment of neuropathic pain, could be encapsulated in liposome for improved oral bioavailability. The excellent IVIVC of capsaicin-loaded liposome could also be a promising tool in liposomal formulation development with an added advantage of reduced animal testing.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Zhu
authors.forename: Miaomiao
authors.initials: M
authors.lastname: Wang
authors.forename: Jiajia
authors.initials: J
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Peng
authors.forename: Caleb Kesse
authors.initials: CK
authors.lastname: Firempong
authors.forename: Wenwen
authors.initials: W
authors.lastname: Deng
authors.forename: Qilong
authors.initials: Q
authors.lastname: Wang
authors.forename: Shicheng
authors.initials: S
authors.lastname: Wang
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Jiangnan
authors.initials: J
authors.lastname: Yu
authors.forename: Ximing
authors.initials: X
authors.lastname: Xu
authors.forename: Weiming
authors.initials: W
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002211:Capsaicin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D065546:Drug Liberation / Q000187:drug effects* / Q000502:physiology; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D008081:Liposomes; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D008081:Liposomes; D002211:Capsaicin