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The purpose of this manuscript was to develop and optimize Fenticonazole Nitrate (FTN)-loaded novasomes aiming to enhance drug corneal penetration and to improve its antifungal activity. Ethanol injection was used to formulate FTN-loaded novasomes adopting a central composite design. The researched factors were: stearic acid concentration (g%) (A), span 80: drug ratio (B) and cholesterol amount (mg) (C), and their effects on percent entrapment efficiency (EE%), particle size (PS), poly-dispersity index (PDI), zeta potential (ZP), and in vitro drug release after 8 hours (Q8h) were studied. Numerical optimization by Design-Expert® software was employed to select the optimum formula in respect to highest EE%, ZP (as absolute value), and Q8h >80% and lowest PS and PDI. Additional evaluation of the optimum formula was accomplished by short term stability study, effect of gamma sterilization, determination of Minimal Inhibitory Concentration and ex vivo corneal permeation study. The in vivo evaluation of the optimum formula was done to ensure its safety via in vivo ocular irritancy and in vivo corneal tolerance studies. Also, the efficacy was confirmed through in vivo corneal uptake study and susceptibility test. The optimum formula with the highest desirability value (0.738) showed EE% (94.31%), PS (197.05 nm), ZP (-66.95 mV) and Q8h (85.33%). It revealed to be safe, with augmented corneal permeation (527.98 µg/cm 2 ) that leads to higher antifungal activity. The above results confirmed the validity of novasomes to improve the corneal permeation and antifungal activity of Fenticonazole Nitrate.

The human eye is a sophisticated organ with distinctive anatomy and physiology that hinders the passage of drugs into targeted ophthalmic sites. Effective topical administration is an interest of scientists for many decades. Their difficult mission is to prolong drug residence time and guarantee an appropriate ocular permeation. Several ocular obstacles oppose effective drug delivery such as precorneal, corneal, and blood-corneal barriers. Routes for ocular delivery include topical, intravitreal, intraocular, juxtascleral, subconjunctival, intracameral, and retrobulbar. More than 95% of marketed products exists in liquid state. However, other products could be in semi-solid (ointments and gels), solid state (powder, insert and lens), or mixed (in situ gel). Nowadays, attractiveness to nanotechnology-based carries is resulted from their capabilities to entrap both hydrophilic and lipophilic drugs, enhance ocular permeability, sustain residence time, improve drug stability, and augment bioavailability. Different in vitro, ex vivo, and in vivo characterization approaches help to predict the outcomes of the constructed nanocarriers. This review aims to clarify anatomy of the eye, various ocular diseases, and obstacles to ocular delivery. Moreover, it studies the advantages and drawbacks of different ocular routes of administration and dosage forms. This review also discusses different nanostructured platforms and their characterization approaches. Strategies to enhance ocular bioavailability are also explained. Finally, recent advances in ocular delivery are described. Graphical Abstract

Photodynamic therapy (PDT) is regarded as a treatment option for basal cell carcinoma (BCC). The aim of this study is to investigate the efficacy of methylene blue (MB)-based PDT in patients suffering from nodular or ulcerative BCCs. This study is a prospective clinical trial with a 6-months follow-up. The study setting is at the Dermatology Clinic at NILES, Cairo University, Egypt. Seventeen patients complaining of nodular BCC (nBCC) and three patients complaining of ulcerative BCC (uBCC) were taken as samples. Methylene blue, the photosensitizer, was prepared in two different formulas: liposomal-loaded MB (LMB) was prepared and formulated in hydrogel (MB 0.2%) to be used topically alone for treating BCCs <2 cm in diameter or to be combined with intralesional injection (ILI) of free MB 2% aqueous solution for treating BCCs ≥2 cm in diameter. A session was performed every 2 weeks until complete response (CR) of the lesion or for a maximum of six sessions. Clinical assessments of clinical improvement, dermatological photography, monthly follow-up visits for 6 months, and skin biopsy after 3 months of follow-up to confirm the response, recurrence, or both in cases in which the clinical evaluation was ambiguous. Seventeen patients of the 20 completed the study, 11 patients achieved CR with very good cosmetic outcome, photosensitizer tolerance, and minimal reported side effects. MB is a cheap promising alternative photosensitizer for PDT of nBCC.