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Backgrounds: A new generic formulation of 3.5% lidocaine hydrochloride ophthalmic gel has been developed in China. This study aimed to evaluate the pharmacokinetics and effectiveness of this lidocaine hydrochloride gel for ocular surface anesthesia. Methods: In the pharmacokinetics study, the new form of 3.5% lidocaine hydrochloride gel or Akten™ 3.5% lidocaine hydrochloride gel was applied in eyes of 70 rabbits. The ocular tissues and plasma samples were collected after the application of 3.5% lidocaine hydrochloride gel or Akten lidocaine gel and analyzed using the liquid chromatography with tandem mass spectrometry (LC-MS/MS) method to determine the concentration of lidocaine. A multicenter, randomized, double-blind prospective clinical trial was conducted in Chinese adults. Two hundred twenty participants were 1:1 randomized into the sham gel group or the lidocaine hydrochloride group. The primary efficacy endpoint was defined as the percentage of subjects achieving anesthesia by 5 min. Results: The animal pharmacokinetics study showed the lidocaine level was significantly higher in the choroid at 15 min and the vitreous body at 15 and 30 min; it was lower in tears at 8 h for 3.5% lidocaine hydrochloride gel than Akten (P ≤ 0.05). Our clinical trial showed that the percentage of subjects achieving anesthesia within 5 min in the lidocaine hydrochloride gel group was significantly higher than the sham gel group (86.92%-18.18%, P < 0.0001). The incidence of adverse events was relatively low and favorable for both groups. Conclusion: This new formulation of lidocaine hydrochloride gel, with pharmacokinetics similar to Akten, may exert a sustained, effective, and safe anesthetic effect. The clinical trial for this new generic formulation of lidocaine hydrochloride has been registered with the Drug Clinical Trial Registration and Information Publicity Platform established by State Food and Drug Administration of China (Registration No. CTR20160593). [ABSTRACT FROM AUTHOR]

Purpose: To design an MG132-sustained drug delivery capsular ring (SDDCR) and investigate its effect on the inhibition of posterior capsule opacification (PCO) in a rabbit model.Methods: The SDDCRs were prepared by forming a slice of film made by the mixture of poly lactic-co-glycolic acid (PLGA) and MG132 on the surface of capsular tension rings (CTRs). The drug-loading capacity, entrapment efficiency, and in vitro release of the drug-containing film were detected. Eighteen New Zealand white rabbits were operated with phacoemulsification and MG132-SDDCRs/PLGA-CTRs/CTRs implantation in the single eye. The images of the anterior segments were acquired at certain days, and the epithelial-mesenchymal transition (EMT) markers were detected by western blot and immunofluorescence.Results: The drug-loading capacity and entrapment efficiency of MG132-SDDCRs were 1.15% ± 0.04% and 66.16% ± 0.027%, respectively, and the drug released well within a month. The PCO degree of the MG132-SDDCR group was significantly lower than the other groups. The expression of alpha-smooth muscle actin, fibronectin, vimentin, and collagen-I was lower, and the expression of E-cadherin (E-cad) was higher in the MG132-SDDCR group than the other groups.Conclusions: MG132-SDDCRs could be established successfully. The PCO process was prevented, and the expression of EMT markers was inhibited by the implantation of MG132-SDDCRs, indicating that this could be a potential treatment against PCO. [ABSTRACT FROM AUTHOR]

Purpose: To compare the effects of topical nonsteroidal anti-inflammatory drugs on pupil dilation maintenance during phacoemulsification cataract surgery and quantify the relationships between pupil size change and nuclear hardness. Methods: This prospective randomized clinical observation study was single centered and double-masked. We studied 239 cases undergoing uneventful phacoemulsification cataract surgery in the absence of significant ocular comorbidity. Cases were randomly assigned to 1 of 6 groups receiving the following treatments: (1) diclofenac (0.1%); (2) pranoprofen (0.1%); (3) control, physiological normal saline solution; (4) diclofenac (0.1%) and epinephrine; (5) pranoprofen (0.1%) and epinephrine; (6) control, physiological normal saline and epinephrine solutions. Pupil diameter was measured at 3 intervals of cataract surgery: before the first incision, at the end of nucleus fragmentation, and at the end of cortex irrigation/aspiration. Results: Compared with patients who were not treated, there was a significant difference in maintaining pupil dilation throughout the operation when the patients were treated with either diclofenac or pranoprofen, P<0.001 and P<0.03, respectively. From the first incision to postnucleus fragmentation, the change in pupil size in both diclofenac and control groups was significantly associated with the hardness of the crystalline lens, P=0.001 and P=0.012, respectively. At the end of irrigation/aspiration, the change in pupil size in only the control groups was significantly associated with the hardness of the crystalline lens, P=0.022. Diclofenac treatment was most effective at inhibiting pupil miosis when the hardness of the nucleus was grade 3, P=0.009. Pupil miosis was not related to the hardness of the nucleus when the patients were treated with epinephrine. Conclusions: Both diclofenac and pranoprofen treatment inhibit surgical-induced miosis. There is a negative correlation between the hardness of the crystalline lens and pupil diameter maintenance at the early stage of phacoemulsification. [ABSTRACT FROM AUTHOR]