title: Improved absorption of salmon calcitonin by ultraflexible liposomes through intranasal delivery.
abstract: The objective of this work was to explore the potential of ultraflexible liposomes as carriers for improving the absorption of salmon calcitonin (sCT) through intranasal administration. The average diameters of positively charged ultraflexible liposomes ranged from about 73 to 99 nm, while those of negatively charged ones were 114 and 157.6 nm, respectively. The content of sodium deoxycholate in liposomes markedly affected the size and encapsulated efficiency of liposomes. The absorption of sCT through intranasal administration was evaluated by hypocalcemic efficacy in rats. The total Ca decrease D% of sCT-loaded ultraflexible liposomes with positive and negative charges were significantly bigger than that of sCT solution, while there was no significant difference in the hypocalcemic efficacy between plain liposome and sCT solution. Unexpectedly, the hypocalcemic efficacy of sCT-loaded ultraflexible liposomes with positive charges was not significantly better than those with negative charges. The decrease rate and extent of the serum calcium level for subcutaneous injection of sCT solution were almost equivalent to those for intranasal administration of negatively and positively charged ultraflexible liposomes within the first 2h, indicating that the ultraflexible liposomes could quickly enhance the penetration of the drug during their residence in the nasal cavity. The results of the toxicity of sCT-loaded ultraflexible liposomes to nasal mucosa demonstrated that the ultraflexible liposomes exerted slight toxicity on the nasal mucosa. On an overall evaluation, the ultraflexible liposomes may be a useful vehicle for intranasal delivery of sCT.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Ming
authors.initials: M
authors.lastname: Chen
authors.forename: Xin-Ru
authors.initials: XR
authors.lastname: Li
authors.forename: Yan-Xia
authors.initials: YX
authors.lastname: Zhou
authors.forename: Ke-Wei
authors.initials: KW
authors.lastname: Yang
authors.forename: Xing-Wei
authors.initials: XW
authors.lastname: Chen
authors.forename: Qiu
authors.initials: Q
authors.lastname: Deng
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.forename: Li-Jun
authors.initials: LJ
authors.lastname: Ren
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D002116:Calcitonin / Q000008:administration & dosage* / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D004337:Drug Carriers; D008081:Liposomes; C028815:salmon calcitonin; D002116:Calcitonin