The objective of this study was to develop a novel hybrid genipin-crosslinked dual-sensitive hydrogel/nanostructured lipid carrier(NLC) drug delivery platform. An ophthalmic antiinflammatory drug, baicalin(BN) was cho...The objective of this study was to develop a novel hybrid genipin-crosslinked dual-sensitive hydrogel/nanostructured lipid carrier(NLC) drug delivery platform. An ophthalmic antiinflammatory drug, baicalin(BN) was chosen as the model drug. BN –NLC was prepared using melt-emulsification combined with ultra-sonication technique. Additionally, a dual pH-and thermo-sensitive hydrogel composed of carboxymethyl chitosan(CMCS) and poloxamer 407(F127) was fabricated by a cross-linking reaction with a nontoxic crosslinker genipin(GP). GP-CMCS/F127 hydrogel was characterized by FTIR, NMR, XRD and SEM. The swelling studies showed GP-CMCS/F127 hydrogel was both pH-and thermo-sensitive. The results of in vitro release suggested BN –NLC gel can prolong the release of baicalin comparing with BN eye drops and BN –NLC. Ex vivo cornea permeation study was evaluated using Franz diffusion cells. The apparent permeability coefficient(Papp) of BN –NLC gel was much higher(4.46-fold) than that of BN eye drops. Through the determination of corneal hydration levels, BN –NLC gel was confirmed that had no significant irritation to cornea. Ex vivo precorneal retention experiments were carried out by a flow-through approach. The results indicated that the NLC-based hydrogel can prolong precorneal residence time. In conclusion, the hybrid NLCbased hydrogel has a promising potential for application in ocular drug delivery.展开更多
Various semi-interpenetrating polymer network（semi-IPN） hydrogels composed of pore-forming agent polyethylene glycol（PEG）, acrylic acid（AA） and acrylamide（AM） were prepared by using free radical polymerization...Various semi-interpenetrating polymer network（semi-IPN） hydrogels composed of pore-forming agent polyethylene glycol（PEG）, acrylic acid（AA） and acrylamide（AM） were prepared by using free radical polymerization with a two-step method. The chemical structures of the synthesized hydrogels were characterized by FTIR spectroscopy and the morphologies were studied by scanning electron microscopy（SEM） method. The swelling properties, such as the p Hresponsive behavior, salt sensitivity, oscillatory swelling/de-swelling behaviors in different solutions with various p H values and self-oscillating behaviors in bath p H oscillator were investigated in detail. The results revealed that the prepared hydrogels exhibited high p H sensitivity and excellent salt sensitivity when the p H values of the medium changes from 3.0 and 7.0 and well reversible properties by undergoing a number of swelling/de-swelling recycles. In particular, the hydrogels exhibited self-oscillation behavior in a closed system containing Br O3？-SO32？-Fe（CN）64？-H＋. This study may create a new possibility as biomaterial for new self-walking actuators and other devices.展开更多
基金National Natural Science Foundation of China (projects 81473163 and 81773670) for supporting the research
文摘The objective of this study was to develop a novel hybrid genipin-crosslinked dual-sensitive hydrogel/nanostructured lipid carrier(NLC) drug delivery platform. An ophthalmic antiinflammatory drug, baicalin(BN) was chosen as the model drug. BN –NLC was prepared using melt-emulsification combined with ultra-sonication technique. Additionally, a dual pH-and thermo-sensitive hydrogel composed of carboxymethyl chitosan(CMCS) and poloxamer 407(F127) was fabricated by a cross-linking reaction with a nontoxic crosslinker genipin(GP). GP-CMCS/F127 hydrogel was characterized by FTIR, NMR, XRD and SEM. The swelling studies showed GP-CMCS/F127 hydrogel was both pH-and thermo-sensitive. The results of in vitro release suggested BN –NLC gel can prolong the release of baicalin comparing with BN eye drops and BN –NLC. Ex vivo cornea permeation study was evaluated using Franz diffusion cells. The apparent permeability coefficient(Papp) of BN –NLC gel was much higher(4.46-fold) than that of BN eye drops. Through the determination of corneal hydration levels, BN –NLC gel was confirmed that had no significant irritation to cornea. Ex vivo precorneal retention experiments were carried out by a flow-through approach. The results indicated that the NLC-based hydrogel can prolong precorneal residence time. In conclusion, the hybrid NLCbased hydrogel has a promising potential for application in ocular drug delivery.
基金financially supported by the Basic Project of Science and Research of Colleges and Universities of Gansu Province(No.5001-109)the Natural Science Foundation of Gansu Province(No.1010 RJZA015)
文摘Various semi-interpenetrating polymer network（semi-IPN） hydrogels composed of pore-forming agent polyethylene glycol（PEG）, acrylic acid（AA） and acrylamide（AM） were prepared by using free radical polymerization with a two-step method. The chemical structures of the synthesized hydrogels were characterized by FTIR spectroscopy and the morphologies were studied by scanning electron microscopy（SEM） method. The swelling properties, such as the p Hresponsive behavior, salt sensitivity, oscillatory swelling/de-swelling behaviors in different solutions with various p H values and self-oscillating behaviors in bath p H oscillator were investigated in detail. The results revealed that the prepared hydrogels exhibited high p H sensitivity and excellent salt sensitivity when the p H values of the medium changes from 3.0 and 7.0 and well reversible properties by undergoing a number of swelling/de-swelling recycles. In particular, the hydrogels exhibited self-oscillation behavior in a closed system containing Br O3？-SO32？-Fe（CN）64？-H＋. This study may create a new possibility as biomaterial for new self-walking actuators and other devices.
