Preparation and evaluation of a contact lens vehicle for puerarin delivery.
The purpose of this study is to develop a soft contact lens vehicle for puerarin delivery to alleviate glaucoma. Poly(2-hydroxy-ethyl methacrylate-co-N-vinylpyrrolidone-co-methyl acrylate) (pHEMA-NVP-MA) contact lenses were prepared by UV irradiation of HEMA, NVP and MA, to which the cross-linker, a mixture of trimethylolpropane trimethacrylate (TMPTMA) and allyl methacrylate (AMA) (1:1, w/w) was added previously. The contact lenses were characterized by equilibrium swelling ratio (ESR) and tensile tester. The results showed that incorporation of poly-N-vinylpyrrolidone (PVP) component in the hydrogels caused increase of ESR and decrease of tensile strength. Co-polymerization of MA monomer in the hydrogel led to a slight drop of ESR and improved tensile strength of hydrogel. Four kinds of hydrated contact lenses with different PVP content were presoaked in PBS solution of puerarin and the in vitro drug release was measured. The contact lenses matrix incorporated with PVP had a remarkable loading capacity of puerarin. In rabbit eyes, the presoaked contact lenses extended the mean resident time of puerarin to 77.45 min from 12.88 min of 1% puerarin eye drops. Moreover, contact lens presoaked in puerarin solution at the concentration of 0.802 mg/ml showed about the same bioavailability (AUC(0-t)) in tear fluid as that of the puerarin eye drops. This kind of presoaked contact lens has potential application as vehicle of puerarin to alleviate glaucoma.
Xu
Jinku
J
Biomaterials and Drug Delivery Laboratories, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, P.R. China.
Li
Xinsong
X
Sun
Fuqian
F
D000179:Acrylates / Q000737:chemistry; D000818:Animals; D003261:Contact Lenses; D016503:Drug Delivery Systems; D005123:Eye / Q000378:metabolism; D005901:Glaucoma / Q000188:drug therapy*; D020100:Hydrogels / Q000737:chemistry*; D007529:Isoflavones / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008422:Materials Testing; D011102:Polyhydroxyethyl Methacrylate / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D011760:Pyrrolidinones / Q000737:chemistry; D011817:Rabbits; D013314:Stress, Mechanical; D013666:Tears / Q000378:metabolism; D014665:Vasodilator Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics
D000179:Acrylates; D020100:Hydrogels; D007529:Isoflavones; D011760:Pyrrolidinones; D014665:Vasodilator Agents; D011102:Polyhydroxyethyl Methacrylate; C042670:N-vinyl-2-pyrrolidinone; D011205:Povidone; C035956:methyl acrylate; C033607:puerarin