The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q₂) and hexagonal (H₂) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, small-angle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3m-type Q₂ and H₂ phase, and both of them showed pseudoplastic fluid properties based on characterization techniques. In vitro release profiles suggested that PN could be sustainably released from LC gels within 48 h. Compared with eye drops, Q₂ and H₂ gel produces a 5.25-fold and 6.23-fold increase in the P_app value (p < .05), respectively, leading to a significant enhancement of corneal penetration. Furthermore, a good biocompatibility and longer residence time on precorneal for LC gels confirmed by in vivo animal experiment. Pharmacokinetic studies showed that LC gels could maintain PN concentration in aqueous humor for at least 12 h after administration and remarkably improve the bioavailability of drug. Additionally, in vivo pharmacodynamics studies indicated that LC gels had a more significant intraocular pressure-lowering and miotic effect compared to eye drops. These research findings hinted that LC gels would be a promising pharmaceutical strategy for ocular application to enhance the efficacy of anti-glaucoma.

Objective: The purpose of this study is to research the mechanism of percutaneous penetration of Ibuprofen (IBU) nanoemulsion. Method: Transdermal penetration mechanism of IBU n anoemulsion was investigated by Fourier Transform infra-Red spectral analysis (FTIR), Differential Scanning Calorimeter thermogram (DSC), activation energy(Ea) measurement The in vivo skin penetration test of rats was carried out using Rhodamine B nanoemulsion to simulate the process of drug penetration into the skin, and the frozen section of the skin was observed by Confocal laser scanning microscopy (CLSM). Result: FTIR spectra and DSC thermogram of rat skin treated with IBU nanoemulsion showed that infiltration occurred due to disruption of the SC protein-lipid structure and increasing of fluidity, hydration and disruption the lipid bilayer structure of the stratum corneum (SC). The significant reduce in Ea (1.255 kcal/mol) for IBU permeating rat skin suggested crucial disruption of the SC lipid bilayers(P < 0.05), which is speculated that nanoemulsion may create new pathways to promote drug penetration. CLSM revealed that Rhodamine B penetrated into the SC in a shorter period of time and it accumulated around the sebaceous glands. Conclusion: The study of skin penetration mechanism indicated that nanoemulsion can be perfectly well used as the transdermal penetration of poorly soluble drugs.