title: Preparation and in vitro characterization of thermosensitive and mucoadhesive hydrogels for nasal delivery of phenylephrine hydrochloride.
abstract: The aim of the present work was to develop a nasal delivery system of phenylephrine hydrochloride (PE) in spray form to make prolonged remedy of nasal congestion. The formulations contain the thermosensitive hydrogel, i.e., Poloxamer 407 (P407) and Poloxamer 188 (P188) mixtures, and mucoadhesives, i.e., ε-polylysine (ε-PL) and low molecular weight sodium hyaluronate (MW 11,000Da). The in vitro characterizations of formulations including rheology studies, texture profiles and in vitro mucoadhesion potential were investigated after gelation temperatures measurements. The results showed that the concentration of P407 or P188 had significant influence on gelation temperature and texture profiles. The addition of mucoadhesives, though lowered the gel strength of formulations, increased interaction with mucin. After screening, two formulations (i.e., 1.0% PE/0.5% ε-PL/17% P407/0.5% P188 or Formulation A; and 1.0% PE/0.5% HA/17% P407/0.8% P188 or Formulation B) presenting suitable gelation temperatures (∼32°C) were used for further studies on in vitro release behaviors and mucosa ciliotoxicity. Both formulations showed sustained release of PE for up to 8h and similar toxicity to saline, the negative control. Thus, the thermosensitive and mucoadhesive PE-containing hydrogels are promising to achieve prolonged decongestion in nasal cavity.
authors.affiliation: State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
authors.forename: Xiaofeng
authors.initials: X
authors.lastname: Xu
authors.affiliation: State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Shen
authors.affiliation: Shanghai Johnson & Johnson Pharmaceuticals, Ltd., Minhang, Shanghai, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
authors.forename: Chunmeng
authors.initials: C
authors.lastname: Sun
authors.affiliation: State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
authors.forename: Chang
authors.initials: C
authors.lastname: Li
authors.affiliation: State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China. Electronic address: xiongyerongcpu@163.com.
authors.forename: Yerong
authors.initials: Y
authors.lastname: Xiong
authors.affiliation: State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, China. Electronic address: jiashengtu@aliyun.com.
authors.forename: Jiasheng
authors.initials: J
authors.lastname: Tu
mesh_terms: D000269:Adhesives / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000378:metabolism; D000281:Administration, Intranasal; D000818:Animals; D001001:Anura; D016503:Drug Delivery Systems / Q000379:methods*; D020100:Hydrogels / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000378:metabolism; D009092:Mucous Membrane / Q000187:drug effects / Q000378:metabolism; D010656:Phenylephrine / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000378:metabolism; D013552:Swine; D013696:Temperature
chemical_list: D000269:Adhesives; D020100:Hydrogels; D010656:Phenylephrine
keywords: Mucoadhesive; Nasal spray; Phenylephrine hydrochloride; Poloxamer; Sodium hyaluronate; Thermosensitive hydrogel; ε-polylysine