title: Preparation and In Vitro-In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability.
abstract: Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and anti-inflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets of capsaicin to enhance its oral bioavailability. The pellets comprised of a core of solid-dispersed capsaicin mixed with microcrystalline cellulose (MCC) and hydroxypropyl cellulose (HPMC) and subsequently coating with ethyl cellulose (EC) were obtained by using the technology of extrusion/spheronization. The physicochemical properties of the pellets were evaluated through scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD). Besides, the in vitro release, in vivo absorption, and in vitro-in vivo correlation were also assessed. More importantly, the relative bioavailability of the sustained-release matrix pellets was studied in fasted rabbits after oral administration using free capsaicin and solid dispersion as references. The oral bioavailability of the matrix pellets and sustained-release matrix pellets of capsaicin was improved approximately 1.98-fold and 5.34-fold, respectively, compared with the free capsaicin. A good level A IVIVC (in vitro-in vivo correlation) was established between the in vitro dissolution and the in vivo absorption of sustained-release matrix pellets. All the results affirmed the remarkable improvement in the oral bioavailability of capsaicin owing to the successful preparation of its sustained-release matrix pellets.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: Ya
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: Zhimin
authors.initials: Z
authors.lastname: Huang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: E
authors.initials: E
authors.lastname: Omari-Siaw
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Lu
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Zhu
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: Dongmei
authors.initials: D
authors.lastname: Jiang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: Miaomiao
authors.initials: M
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
authors.forename: Jiangnan
authors.initials: J
authors.lastname: Yu
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China. xmxu@ujs.edu.cn.
authors.forename: Ximing
authors.initials: X
authors.lastname: Xu
authors.affiliation: Nanjing Institute for Comprehensive Utilization of Wild Plants, Nanjing, 210042, China. botanyzh@163.com.
authors.forename: Weiming
authors.initials: W
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002211:Capsaicin / Q000737:chemistry* / Q000493:pharmacokinetics*; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000493:pharmacokinetics*; D004343:Drug Implants / Q000737:chemistry* / Q000493:pharmacokinetics*; D005079:Excipients / Q000737:chemistry; D008297:Male; D008855:Microscopy, Electron, Scanning / Q000379:methods; D011817:Rabbits; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D000893:Anti-Inflammatory Agents; D003692:Delayed-Action Preparations; D004343:Drug Implants; D005079:Excipients; C013517:ethyl cellulose; D002482:Cellulose; C008079:hydroxypropylcellulose; C109691:microcrystalline cellulose; D002211:Capsaicin
keywords: capsaicin; in vitro release; oral bioavailability; pharmacokinetic studies; sustained-release pellets