Navigating Skin Delivery Horizon: An Innovative Approach in Pioneering Surface Modification of Ultradeformable Vesicles.

In the dynamic landscape of pharmaceutical advancements, the strategic application of active pharmaceutical ingredients to the skin through topical and transdermal routes has emerged as a compelling avenue for therapeutic interventions. This non-invasive approach has garnered considerable attention in recent decades, with numerous attempts yielding approaches and demonstrating substantial clinical potential. However, the formidable barrier function of the skin, mainly the confinement of drugs on the upper layers of the stratum corneum, poses a substantial hurdle, impeding successful drug delivery via this route. Ultradeformable vesicles/carriers (UDVs), positioned within the expansive realm of nanomedicine, have emerged as a promising tool for developing advanced dermal and transdermal therapies. The current review focuses on improving the passive dermal and transdermal targeting capacity by integrating functionalization groups by strategic surface modification of drug-loaded UDV nanocarriers. The present review discusses the details of case studies of different surface-modified UDVs with their bonding strategies and covers the recent patents and clinical trials. The design of surface modifications holds promise for overcoming existing challenges in drug delivery by marking a significant leap forward in the field of pharmaceutical sciences.

Unlocking the Potential of Bilosomes and Modified Bilosomes: a Comprehensive Journey into Advanced Drug Delivery Trends.

Vesicular drug delivery systems have revolutionized the pharmaceutical field, offering a promising path for achieving targeted and sustained drug delivery. The oral, transdermal, and ocular routes of administration offer optimal ease in attaining desired therapeutic outcomes. However, conventional treatment strategies are all plagued with several challenges, such as poor skin permeability, ocular barriers, and gastrointestinal (GIT) degradation leading to vesicular disruption with the release of the encapsulated drug before reaching the targeted site of action. In recent years, bilosomes-stabilized nanovesicles containing bile salts have received considerable attention due to their versatility and adaptability for diverse applications. These bilayered vesicles enhance the solubility of lipophilic drugs and improve formulation stability in the gastrointestinal tract. They exhibit ultra-deformable properties, improving stratum corneum permeability, making them ideal candidates for oral and transdermal drug delivery. In addition, bilosomes find utility in topical drug delivery, making them applicable for ocular administration. Over the past decade, extensive research has highlighted bilosomes' potential as superior vesicular carriers surpassing liposomes and niosomes. Advances in this field have led to the development of modified bilosomes, such as probilosomes and surface-modified bilosomes, further enhancing their capabilities and therapeutic potential. Thus, the present review provides a comprehensive summary of bilosomes, modified bilosomes, surface modifications with their mechanism of action, formulation components, preparation methods, patents, and a wide array of recent pharmaceutical applications in oral, transdermal, and ocular drug delivery. The enhanced properties of bilosomes offer promising prospects for targeted and effective drug delivery, providing potential solutions for addressing various therapeutic challenges.

A Comprehensive Review on Preparation, Evaluation and Applications of Deformable Liposomes.

Elastic or deformable liposomes are phospholipid-based vesicular drug delivery systems that help improve the delivery of therapeutic agents through the intact skin membrane due to their deformable characteristics that overcome the problems of conventional liposomes. In the present review, different types of deformable liposomes such as transfersomes, ethosomes, menthosomes, invasomes and transethosome are studied, and their mechanism of action, characterization, preparation methods, and applications in pharmaceutical technology through topical, transdermal, nasal and oral routes for effective drug delivery are compared for their potential transdermal delivery of poorly permeable drugs. Due to the deformable characteristics of these vehicles, it resulted in modulation of increased drug encapsulation efficiency, permeation and penetration of the drug into or through the skin membrane and are found to be more effective than conventional drug delivery systems. So deformable liposomes can, therefore, be considered as a promising way of delivering the drugs transdermally.

Formulation, Optimization and Evaluation of Novel Ultra-deformable Vesicular Drug Delivery System for an Anti-fungal Drug.

The present study is aimed at enhancing the skin penetration of ketoconazole by formulating it as transethosome. Ketoconazole-loaded transethosome formulations were prepared by conventional thin film evaporation and hydration method and were optimized using concentration of edge activator (span 80), ethanol and sonication time as factors and particle size, polydispersity index and entrapment efficiency as responses. The optimized formulation was further evaluated for in vitro diffusion, anti-fungal activity, ex vivo penetration and in vivo pharmacodynamic activity. The results of in vitro drug diffusion and ex vivo skin penetration studies demonstrated that the amount of drug diffused and penetrated through the skin was increased. Optimized transethosomes showed enhanced in vitro antifungal and in vivo pharmacodynamic activities against Candida albicans in Wistar albino rats when compared to conventional liposomes. Therefore, the developed ketoconazole encapsulated transethosome formulation is capable of enhancing the skin penetration of the drug by overcoming the stratum corneum barrier function and acting as an effective drug delivery system for ketoconazole through the skin for its anti-fungal activity.