Formulation and Characterization of Oleogel as a Topical Carrier of Azithromycin.

This study aims to formulate azithromycin oleogel to locally treat skin infections such as acne vulgaris and skin wound infection. Providing a form of azithromycin that can be administered topically is highly desired to prevent unwanted systemic complications including diarrhea, nausea, and abdominal pain. Additionally, it will avoid first pass metabolism, improves patient acceptance, provides an alternative in nauseated patients, decreases the dose by direct contact with the pathological site, and provides a noninvasive and convenient mode of administration. Furthermore, for treating wound infections, the gel will act as a scaffold biomaterial for wound closure besides its antibacterial effect. Herein, we propose the use of grapeseed oil-based oleogel with glycerol monostearate (GMS) as an organogelator as a promising strategy for the effective topical delivery of azithromycin. A series of oleogels were prepared by varying concentrations of organogelators namely GMS, palmitic acid, Compritol 888, and stearic acid, while maintaining the weight ratio of grapeseed oil and clove oil constant. Initial evaluation showed azithromycin oleogel with 15% GMS to be the optimum formulation and it was selected for further evaluation. In vivo testing of the formulated gel showed significant effectiveness in promoting faster clinical healing of Staphylococcus aureus infected wounds. The findings of the present study suggest that azithromycin oleogel is stable, safe, cost-effective, and it provides significant antibacterial activity.

Ocular Drug Delivery Barriers-Role of Nanocarriers in the Treatment of Anterior Segment Ocular Diseases.

Ocular drug delivery is challenging due to the presence of anatomical and physiological barriers. These barriers can affect drug entry into the eye following multiple routes of administration (e.g., topical, systemic, and injectable). Topical administration in the form of eye drops is preferred for treating anterior segment diseases, as it is convenient and provides local delivery of drugs. Major concerns with topical delivery include poor drug absorption and low bioavailability. To improve the bioavailability of topically administered drugs, novel drug delivery systems are being investigated. Nanocarrier delivery systems demonstrate enhanced drug permeation and prolonged drug release. This review provides an overview of ocular barriers to anterior segment delivery, along with ways to overcome these barriers using nanocarrier systems. The disposition of nanocarriers following topical administration, their safety, toxicity and clinical trials involving nanocarrier systems are also discussed.

Formulation and In Vitro Evaluation of Cyclosporine-A Inserts Prepared Using Hydroxypropyl Methylcellulose for Treating Dry Eye Disease.

PURPOSE: The aim of this study was to develop and characterize a novel sustained-release drug delivery system of cyclosporine-A (CsA) using hydroxypropyl methylcellulose (HPMC) and xanthan gum (XG) for treating dry eye disease (DED). METHODS: Polymeric inserts of CsA were prepared using the solvent casting technique with a 2(3) full factorial design to evaluate the effect of HPMC and XG ratios and drug content on thickness, folding endurance, wettability, and in vitro drug release. Inserts were also evaluated for drug content, moisture absorption and loss, and surface pH. Inserts with an optimized ratio of HPMC and XG were sterilized with UV light and evaluated for morphology, thermal analysis, Fourier transform infrared spectroscopy, stability at 4°C, 25°C, and 40°C, cytotoxicity in cultured bovine corneal endothelial cells, and anti-inflammatory effect in Jurkat T cells. RESULTS: The addition of XG increased the CsA release duration and enhanced the folding endurance of films. All films showed uniformity in drug content and thickness. Formulation F4 composed of 1% HPMC and 0.25% XG exhibited good folding endurance and sustained CsA release for up to 20 h. Sterility testing of F4 using plate and direct inoculation confirmed the formulation sterility and validated the sterilization method. The formulation was stable for at least 3 months at 4°C, 25°C, and 40°C. No cytotoxicity was observed in cultured bovine corneal endothelial cells for up to 24 h. The anti-inflammatory effect of CsA was intact in ophthalmic inserts. CONCLUSION: In conclusion, combination therapy with HPMC and CsA can be a potential once-a-day formulation for treating DED.

Dry Eye Disease: Present Challenges in the Management and Future Trends.

Dry eye disease (DED) is a tear film disorder resulting in hyperosmolarity of the tear film and inflammation of the ocular surface. DED is also referred to as keratoconjunctivitis sicca (KCS) and dry eye syndrome. DED represents a significant public health issue, particularly in older adults, and needs more research and attention. Despite the urgent need for safe and effective pharmacotherapies, there is currently only one approved medication, Restasis®, to tackle DED. In this review article, we present an overview of DED, classification, epidemiology, pathophysiology, diagnosis, and risk factors of DED. Special emphasis is placed on current treatment options for DED such as artificial tears, lipid-containing lubricants, liposomal spray, inserts, anti-inflammatory or immunosuppressant drops, antibiotics, dietary omega-3 essential fatty acids, autologous serum, intense-pulsed-light (IPL), punctual plugs, moisture-retaining eyeglasses, hydrophilic bandage contact lenses and secretagogues. The review also summarizes trends in DED treatment that are patented and are currently under investigation in clinical trials.