Mesoporous silica nanoparticles: An emerging approach in overcoming the challenges with oral delivery of proteins and peptides.

Proteins and peptides (PPs), as therapeutics are widely explored in the past few decades, by virtue of their inherent advantages like high specificity and biocompatibility with minimal side effects. However, owing to their macromolecular size, poor membrane permeability, and high enzymatic susceptibility, the effective delivery of PPs is often challenging. Moreover, their subjection to varying environmental conditions, when administered orally, results in PPs denaturation and structural conformation, thereby lowering their bioavailability. Hence, for effective delivery with enhanced bioavailability, protection of PPs using nanoparticle-based delivery system has gained a growing interest. Mesoporous silica nanoparticles (MSNs), with their tailored morphology and pore size, high surface area, easy surface modification, versatile loading capacity, excellent thermal stability, and good biocompatibility, are eligible candidates for the effective delivery of macromolecules to the target site. This review highlights the different barriers hindering the oral absorption of PPs and the various strategies available to overcome them. In addition, the potential benefits of MSNs, along with their diversifying role in controlling the loading of PPs and their release under the influence of specific stimuli, are also discussed in length. Further, the tuning of MSNs for enhanced gene transfection efficacy is also highlighted. Since extensive research is ongoing in this area, this review is concluded with an emphasis on the potential risks of MSNs that need to be addressed prior to their clinical translation.

Development of a Novel Freeze-dried Mulberry Leaf Extract-based Transfersome Gel.

OBJECTIVES: Nowadays, antioxidants are important for health-related concerns related to acne vulgaris. Acne vulgaris is interrelated with the development of free radicals that interact with cells. Mulberry leaves contain phenolic compounds, including antioxidants such as quercetin. An antioxidant is a scavenger of free radicals. The current study addresses the development of a mulberry leaf extract-based transfersome gel containing quercetin by a thin-layer hydration method for topical antioxidant delivery. The process was optimized by encapsulating the drug in a variety of transfersome formulations. MATERIALS AND METHODS: Batch optimization was carried out by particle size and zeta analysis, entrapment efficiency (%), polydispersity index, in vitro drug release, and drug content analysis. RESULTS: The optimized batch MF5 provided 86.23% entrapment efficiency of quercetin in the vesicles and 95.79% drug release. It furnished a spherical shaped vesicle with an average diameter of 118.7 nm and zeta potential of -45.11 mV. The MG1 formulation provided superior antioxidant activity, drug content, and entrapment efficiency, ex vivo drug release, spreadability, homogeneity, and stability to MG2. The presence of quercetin in the extract and gel formulation was confirmed by using high performance thin layer chromatography. CONCLUSION: It is evident from this study that a mulberry leaf extract-based transfersome gel is a promising prolonged delivery system for quercetin and has reasonably good stability characteristics. This research recommends that mulberry leaf extract-based transfersome gel can potentially be used in the treatment of acne vulgaris through a transdermal drug delivery system.