title: Dissolution and bioavailability of lercanidipine-hydroxypropylmethyl cellulose nanoparticles with surfactant.
abstract: The objective of this study was to develop lercanidipine-hydroxypropylmethyl cellulose (HPMC) nanoparticles with high oral bioavailability. The lercanidipine-HPMC nanoparticles with/without surfactants were manufactured using a supercritical antisolvent (SAS) process. Gelucire 44/14, poloxamer 407, and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were evaluated as surfactants. Spherical lercanidipine-HPMC nanoparticles with a mean particle size less than 400 nm were successfully prepared using a SAS process. The dissolution and oral bioavailability of lercanidipine was significantly increased by addition of surfactants. Especially lercanidipine-HPMC nanoparticles with TPGS showed a 2.47-fold higher oral bioavailability than raw material. Furthermore, the dissolution efficiency was strongly correlated to the in vivo Cmax and AUC0 → 24h. Therefore, the preparation of HPMC nanoparticles with TPGS using a SAS process is a highly effective formulation strategy for enhanced oral bioavailability of lercanidipine.
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Eun-Sol
authors.initials: ES
authors.lastname: Ha
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Gwang-Ho
authors.initials: GH
authors.lastname: Choo
authors.affiliation: College of Pharmacy, Kyungsung University, Daeyeon-dong, Nam-gu, Busan 608-736, Republic of Korea.
authors.forename: In-hwan
authors.initials: IH
authors.lastname: Baek
authors.affiliation: College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Republic of Korea.
authors.forename: Jung-Soo
authors.initials: JS
authors.lastname: Kim
authors.affiliation: College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Republic of Korea; Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea.
authors.forename: Wonkyung
authors.initials: W
authors.lastname: Cho
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Young Suk
authors.initials: YS
authors.lastname: Jung
authors.affiliation: College of Pharmacy, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea.
authors.forename: Su-Eon
authors.initials: SE
authors.lastname: Jin
authors.affiliation: Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea; College of Pharmacy, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea.
authors.forename: Sung-Joo
authors.initials: SJ
authors.lastname: Hwang
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea. Electronic address: minsookim@pusan.ac.kr.
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Kim
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D004095:Dihydropyridines / Q000008:administration & dosage / Q000737:chemistry*; D004339:Drug Compounding; D006801:Humans; D065347:Hypromellose Derivatives / Q000008:administration & dosage / Q000737:chemistry*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D012995:Solubility; D014810:Vitamin E / Q000737:chemistry
chemical_list: D004095:Dihydropyridines; D020442:Poloxamer; C104509:gelucire 44-14; D014810:Vitamin E; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols; C014225:tocophersolan; C060343:lercanidipine
keywords: Bioavailability; Lercanidipine; Nanoparticle