PEG-interpenetrated genipin-crosslinked dual-sensitive hydrogel/nanostructured lipid carrier compound formulation for topical drug administration

• Published in: Artificial cells, nanomedicine, and biotechnology nanomedicine, and biotechnology, 2021-01, Vol.49 (1), p.345-353
• Main Authors: Li, Qijun, Gong, Shiqiang, Yao, Weifan, Yu, Yibin, Liu, Chao, Wang, Renjun, Pan, Hao, Wei, Minjie
• Format: Article
• Language: English
• Subjects: Administration, Topical; Animals; Biocompatibility; carboxymethyl chitosan; Chemical synthesis; Chitosan; Crosslinking; Drug Carriers - chemistry; Drug delivery; Drug delivery systems; Drug Liberation; dual-sensitivity hydrogel; Emulsification; Ethylene glycol; Genipin; Hydrogels; Hydrogels - chemistry; Hydrogels - pharmacology; In vitro methods and tests; Iridoids - chemistry; Lipids; Lipids - chemistry; Lipoic acid; Mechanical properties; Mice; Nanostructures - chemistry; PEG interpenetrated; Physicochemical properties; Poloxamers; Polydispersity; Polyethylene glycol; Polyethylene Glycols - chemistry; Rheological properties; Thioctic Acid - chemistry; topical delivery; Zeta potential
• ISSN: 2169-1401; 2169-141X; 2169-141X
• DOI: 10.1080/21691401.2021.1879104

PEG-interpenetrated dual-sensitive hydrogels that load nano lipid carrier (NLC) were researched and developed for topical drug administration. Natural antioxidant α-lipoic acid (ALA) was selected as our model drug. The α-lipoic acid (ALA) nano lipid carrier was successfully prepared by hot melt emulsification and ultrasonic dispersion method, and the physicochemical properties of the nano lipid carrier were investigated, including morphology, particle distribution, polydispersity coefficient, zeta potential and encapsulation efficiency. Carboxymethyl chitosan and poloxamer 407 contributed to pH- and temperature-sensitive properties in the hydrogel, respectively. Natural non-toxic cross-linking agent genipin reacted with carboxymethyl chitosan to form the hydrogel. Poly ethylene glycol (PEG), a polymer compound with good water solubility and biocompatibility, interpenetrated the hydrogel and influenced the mechanical strength and drug release behaviour. FI-IR test verified the successful synthesis of the hydrogel. The rheological parameters indicated that the mechanical strength of the hydrogel was positively correlated with the amount of PEG, and the in vitro dissolution profiles demonstrated that the increasement of PEG could accelerate the drug release rate. The compatibility of the drug delivery system was verified with cells and mice model. Topical delivery of ALA in solution, NLC and NLC-gel was investigated in-vitro.