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AIDS is one of the world's most serious public health challenges. Protease inhibitors are key components of AIDS treatment regimen. Ritonavir is a well-known protease inhibitor with low aqueous solubility belonging to BCS class II category. Some of the severe adverse effects associated with this drug restricted its use in the treatment of AIDS. However, several attempts were made by researchers in the past to enhance the oral bioavailability of Ritonavir.The current review mainly focuses on the adverse effects of Ritonavir and recent approaches followed by researchers on the development of nanoformulations of Ritonavir. Further, various patents filed on Ritonavir have also been discussed in the current review.Most research on nanoformulation development for Ritonavir is mainly focused on enhancing the solubility and oral bioavailability of the drug. Some of the researchers focused on the lymphatic targeting of the drug in order to bypass the hepatic metabolism of the drug. However, most of the research topics did not cover the toxicity evaluation of the developed formulation. Since the major issue of Ritonavir is not only oral bioavailability but also drug-induced toxicity, this area needs to be considered during the formulation development.

Despite numerous remarkable developments in clinical therapy, the world remains firmly in the grip of fungal infections. While conventional approaches to antifungal therapy are failing, dermatophytes continue to affect people’s daily lives, especially in humid and tropical areas, and pose a major medical problem. Cubosomes, the liquid crystalline nanostructures, are among the recently developed lipid nanoparticles that could potentially overcome the hurdles of conventional therapy. In the present study, cubosomes containing luliconazole, an antifungal drug, were formulated to overcome the limitation of poor water solubility and poor bioavailability of the drug for the main purpose of treating fungal infections. Various formulations of luliconazole loaded cubosomes were prepared with different ratios of lipid (glyceryl monooleate) and surfactant (poloxamer 407) using emulsification method. The prepared formulations were optimised and the optimised cubosomal dispersion was loaded into a carbomer-934 gel to form an emulsifying gel. All cubosomal dispersions had particle sizes ranging from 124 nm to 221.1 nm, optimal zeta potential and polydispersity index, and were found to be stable. The drug entrapment efficiency of the cubosomes was over 90%. The in vitro diffusion study showed that the developed formulation had a higher release rate than the marketed formulation. The in vitro antifungal activity study confirmed that the prepared emulsion formulation was also effective against Candida albicans. The novel drug delivery system developed in this study, the cubosomal emulgel, could thus be a favourable approach for the topical delivery of luliconazole for the treatment of fungal infections.

The aim of the present study was to formulate a fluconazole cream for the treatment of Candida albicans. The optimized cream formulation was prepared using stearic acid, oleic acid, beeswax and borax. The uniform distribution of the active ingredient fluconazole could be confirmed in all formulated creams. The FC-C-C formulation showed satisfactory spreadability and extrudability. FC-C-C delivered (95.07 ± 15.85)% in only 36 h, and the formulation released the drug by an anomalous diffusion mechanism. The viscosity of FC-C-C was found to be (63.20 ± 0.83) cP. The antifungal study and animal studies confirmed that the prepared formulation is non-irritant and has an enhanced antifungal activity that reduces the side effects of fluconazole. The studies confirm that the prepared formulation may be useful for the treatment of Candida albicans.

Background: The formulation of spanlastic vesicles of luliconazole can be used to overcome its poor skin permeation and improve its antifungal efficacy. Objective: In this study, we aimed to enhance the dermal delivery of luliconazole, an antifungal drug, through spanlastic vesicles. Methods: A 23 regular factorial design was employed, using the Design Expert® software for optimization. The independent variables chosen were Span: Edge activator ratio, type of edge activator, and sonication intensity and their effect on the dependent variables, i.e., entrapment efficiency, particle size, and percentage of drug release after 8h were determined. Spanlastics were formulated by ethanol injection method using Tween 80 as an edge activator. Results: Spanlastics were found to possess sizes in the nano range with entrapment efficiencies between 77 - 88% with optimum zeta potential and polydispersity index indicating a stable formulation. Differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared studies revealed complete encapsulation of the drug within the elastic carriers. The optimized spanlastic formulation was further incorporated into a gel base and was found to be sufficiently viscous, spreadable, homogenous, showed a prolonged release for up to 8h and was also found to be non-irritant. The in-vitro permeation study revealed that the flux value obtained for luliconazole entrapped in the vesicular spanlastics (0.2292 mg/cm2.h) was also found to be higher than that of the marketed (0.1302 mg/cm2.h) and conventional gel (0.1122 mg/cm2.h). The optimized gel formulation was also evaluated for its antimycotic activity. Moreover, the optimized gel formulation also possessed a greater antimycotic activity against Candida albicans. The spanlastics loaded hydrogel formulation was found to have a greater zone of inhibition in comparison to the marketed formulation, thus proving to have optimum antifungal activity against Candida albicans. Conclusion: Collectively, the results revealed that spanlastics could be a potential nanocarrier for wellcontrolled delivery and for targeting deeper skin layers, thus providing new opportunities for dermal treatment.

Exosomes are extracellular vesicles with the diameter ranging from 50 to 100 nm and are found in different body fluids such as blood, cerebrospinal fluid (CSF), urine and saliva. Like in case of various diseases, based on the parent cells, the content of exosomes (protein, mRNA, miRNA, DNA, lipids and metabolites) varies and thus can be utilized as potential biomarker for diagnosis and prognosis of the brain diseases. Furthermore, utilizing the natural potential exosomes to cross the blood–brain barrier and by specifically decorating it with the ligand as per the desired brain sites therapeutics can be delivered to brain parenchyma. This review article conveys the importance of exosomes and their use in the treatment and diagnosis of brain/central nervous system diseases. Graphical abstract

With the launch of few products in the market, transdermal drug delivery through microneedles (MNs) has evidenced a major leap. Interest in MNs is growing exponentially as it overcomes the limitations accompanying other delivery routes. Among the various types of MNs, polymeric microneedles (PMNs) seem to be more propitious because of the associated favourable innate properties. Nevertheless, struggle in loading capacity, unmanageable rate of drug release, and monotonic curative approach hampers the further development of PMNs. Recent emerging research has drawn inspiration from nanocarriers and in conjunction with PMNs have opened up new perspectives for the treatment of various diseases. In this review, we focus on recent progresses in the field of transdermal drug delivery using nano carriers in conjunction with PMNs for various therapeutic and diagnostic activities. Additionally, we describe the various factors impacting drug delivery, and challenges involved in sterilization and stability aspects associ ted with nanocarrier loaded PMNs, highlighting future research perspectives alongside.

Felodipine (FDP), a dihydropyridine calcium-channel antagonist is used for the treatment of hypertension and angina pectoris. FDP is poorly soluble drug and upon oral administration, it undergoes first pass metabolism, resulting in bioavailability of 15%. The present work was aimed to formulate rapidly dissolving strips containing FDP nanoparticles for transbuccal administration. Such formulations are absorbed through buccal mucosa resulting in increase in oral bioavailability by circumventing first pass metabolism. Nanosuspension was formulated using solvent-antisolvent sonoprecipitation technique. An ordinary 23 factorial design was applied using Design Expert® 12 software. Formulated nanosuspensions were characterized for particle size, polydispersity index, zeta potential and saturation solubility. Surface morphology was studied using high resolution transmission electron microscopy, atomic force microscopy and field emission scanning electron microscopy. The optimised nanosuspension D1 formulated with PVP-K30 as stabiliser was selected for further incorporation into the film. Central composite design was applied to select film composition with desirable properties. X-ray diffraction studies were performed to assess the solid-state characteristic of the drug in the formulation. Rapidly dissolving strips were evaluated for weight variation, folding endurance, disintegration time, thickness and surface pH. Scanning electron microscopy image of the optimised film revealed almost granular-shaped nanoparticles dispersed in the polymeric network. Drug release kinetics data of optimised film F5 showed 82 ± 0.47% release within 4 min and release pattern was non-fickian diffusion controlled. Stability studies were conducted at 25 ± 2 °C/60 ± 5% RH for 90 days. Collectively, the developed film demonstrated to possess optimum physical and mechanical properties along with rapid drug release and good stability.