title: Transdermal delivery of the in situ hydrogels of curcumin and its inclusion complexes of hydroxypropyl-β-cyclodextrin for melanoma treatment.
abstract: Curcumin (Cur) is a hydrophobic polyphenol with diverse pharmacological effects, especially for cancer treatment. However, its weak water solubility and stability was the major obstacle for the formulation research of Cur. The complexation of Cur and hydroxypropyl-β-cyclodextrin (HP-β-CD) was done by grinding. The increasing solubility of Cur was achieved due to complexation and the photochemical stability of Cur was improved. The inclusion of Cur could happen when two ends of Cur were embedded into the cavity of the HP-β-CD rings. The in situ hydrogels (ISGs) of Cur and its inclusion complexes were prepared using poloxamers 407 and 188 as the matrix. The extent of drug's in vitro release from the ISGs depended on the dissolution of drugs. Both of the ISGs had transdermal effect and cytotoxicity on B16-F10 cells. However, the effects of the ISGs containing Cur inclusion complexes were much higher than those of Cur ISGs because of the improved Cur solubility in the former. The cytotoxicity of Cur on melanoma cells was related to blocking of cellular proliferation in the G2/M stage followed by cellular apoptosis. The ISGs of Cur inclusion complexes are a promising formulation for melanoma treatment.
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors.forename: Yunbo
authors.initials: Y
authors.lastname: Sun
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors.forename: Lina
authors.initials: L
authors.lastname: Du
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors.forename: Yangpu
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Chinese PLA General Hospital, Beijing 100853, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Li
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors.forename: Miao
authors.initials: M
authors.lastname: Li
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, China. Electronic address: jinyg@bmi.ac.cn.
authors.forename: Yiguang
authors.initials: Y
authors.lastname: Jin
authors.affiliation: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Qian
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000279:Administration, Cutaneous; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers; D004355:Drug Stability; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D005782:Gels; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D020442:Poloxamer / Q000737:chemistry; D012878:Skin Neoplasms / Q000188:drug therapy* / Q000473:pathology; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D005782:Gels; D047392:beta-Cyclodextrins; D020442:Poloxamer; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D003474:Curcumin
keywords: Erosion; In situ hydrogels; Inclusion complexes; Melanoma; Transdermal