Mefenamic Acid Loaded and TPGS Stabilized Mucoadhesive Nanoemulsion for the Treatment of Alzheimer's Disease: Development, Optimization, and Brain-Targeted Delivery via Olfactory Pathway.

Alzheimer's disease (AD) is a very common disorder that affects the elderly. There are relatively few medications that can be used orally or as a suspension to treat AD. A mucoadhesive (o/w) nano emulsion of mefenamic acid was made by adding Carbopol 940P to the optimised drug nanoemulsion using distilled water as the aqueous phase (6%); Solutol HS: tween 20 (3.6%) as the surfactant and co-surfactant; and clove oil: TPGS (0.4%) as the oil phase and mefenamic acid as the drug (2.8 mg/ml). The mucoadhesive nanoemulsion (S40.5%w/v) had a particle size of 91.20 nm, polydispersity index of 0.270, and surface charge of - 12.4 mV. Significantly higher (p < 0.001) drug release (89.37%) was observed for mucoadhesive drug formulation in comparison to mucoadhesive drug suspension (25.64%) at 8 h. The ex vivo nasal permeation of 83.03% in simulated nasal fluid and 85.71% in artificial cerebrospinal fluid was observed. The percent inhibition and inhibitory concentration (IC50) of mucoadhesive drug nanoemulsion were found to be 91.57 ± 2.69 and 6.76 respectively. Higher cell viability on glioblastoma cells (85-80%) was researched for mucoadhesive nanoemulsion as compared to drug suspension (80-70%). Significantly higher (p < 0.001) drug absorption and Cmax (491.94 ± 24.13 ng/ml) of mucoadhesive drug nanoemulsion were observed than mucoadhesive drug suspension (107.46 ± 11.46 ng/ml) at 8 h. The stability studies confirmed that the formulation was stable at 40°C ± 2°C and 75 ± 5% RH. The authors concluded that the mucoadhesive mefenamic acid-loaded nanoemulsion may be an effective technique for treating Alzheimer's disease by intranasal route.

Resveratrol-loaded folate targeted lipoprotein-mimetic nanoparticles with improved cytotoxicity, antioxidant activity and pharmacokinetic profile.

The aim of present study was to develop folate receptor targeted lipoprotein-mimetic nanoparticles of resveratrol (RSV). Lipoprotein-mimicking nanocarrier (RSV-FA-LNPs) comprising of phosphatidyl choline, cholesterol, stearyl amine and folic acid-tagged bovine serum albumin (FA-BSA) were prepared. Folic acid was conjugated to bovine serum albumin by amide bond at a binding rate of 9.46 ± 0.49 folate molecules per bovine serum albumin. The particle size and entrapment efficiency of the developed nanoparticles was found to be 291.37 ± 3.81 nm and 91.96 ± 1.83%, respectively. The in vitro release study depicted that developed nanocarrier prolonged the drug release till 72 h in phosphate buffer saline (pH 7.4). The anticancer potential of RSV in case of RSV-FA-LNPs was found to be substantially improved against MCF-7 cells overexpressing folate receptors compared to non-targeted nanoparticles. The pharmacokinetics studies after intravenous administration in healthy Wistar rats depicted that lipoprotein mimicking nanoparticles presented the longer circulation time (>48 h) compared to free drug which disappeared in few hours (6 h). The in vitro and preclinical findings of the present study demonstrated the applicability of lipoprotein mimicking nanocarriers for the safer and effective delivery of bioactives.

Nano-Based Drug Delivery System: Recent Strategies for the Treatment of Ocular Disease and Future Perspective.

The structure of the eye is very complex in nature which makes it a challenging task for pharmaceutical researchers to deliver the drug at the desired sites via different routes of administration. The development of the nano-based system helped in delivering the drug in the desired concentration. Improvement in penetration property, bioavailability, and residence time has all been achieved by encapsulating drugs into liposomes, dendrimers, solid lipid nanoparticle, nanostructured lipid carrier, nanoemulsion, and nanosuspension. This review puts emphasis on the need for nanomedicine for ocular drug delivery and recent developments in the field of nanomedicine along with recent patents published in the past few years.

Nanoformulations for Ocular Delivery of Drugs - A Patent Perspective.

Efficient delivery of ocular therapeutics with improved efficacy, enhanced bioavailability, and acceptable patient compliance presents unique challenges. This can be attributed to the presence of protective mechanisms, physicobiological barriers, and structural obstacles in the eye. Nanotherapeutic interventions have been explored extensively over the past few years to overcome these limitations. The present review focusses on the nanoformulations developed for the diagnosis and treatment of various ocular diseases besides providing an in-depth insight into the patents reported for the same.

Nanostructured lipid carriers: An emerging platform for improving oral bioavailability of lipophilic drugs.

Nowadays exploration of novel lipid-based formulations is akin to a magnet for researchers worldwide for improving the in vivo performance of highly lipophilic drugs. Over the last few years, new compositions of lipids have been developed, and the probable bioavailability enhancement has been investigated. We reviewed the most recent data dealing with backlogs of conventional lipid-based formulations such as physical instability, limited drug loading capacities, drug expulsion during storage along with all the possible hindrances resulting in poor absorption of highly lipophilic drugs such as P-glycoprotein efflux, extensive metabolism by cytochrome P450 etc. In tandem with these aspects, an exclusive formulation approach has been discussed in detail in this paper. Therefore, this review focuses on resolving the concerned ambiguity with successful oral administration of highly lipophilic drugs through designing novel lipidic formulations (nanostructured lipid carriers [NLC]) that constitute a blend of solid and liquid lipids. The article highlights the potential role of such formulation in normalizing the in vivo fate of poorly soluble drugs. Finally, the present manuscript discusses the dominance of NLC over other lipid-based formulations and provides a perspective of how they defeat and overcome the barriers that lead to the poor bioavailability of hydrophobic drugs.

Nanomedicines for dental applications-scope and future perspective.

Nanotechnology is directed at manipulating matter at the nanometer level and the application of the same to medicine is called nanomedicine. Over the past few years researchers have developed various nanomedicines for diagnosis, prevention as well as cure of various ailments both locally and systemically. In dentistry, drug loaded nanopharmaceuticals based on nanomaterials have been utilized extensively over the past few years to cure dental problems and facilitate attainment of a near-perfect oral hygiene. Although various drug delivery systems have already been investigated for treating periodontitis, research is currently focused on nanodelivery systems for efficient targeted delivery of drugs to the periodontal pocket. In this context a few nanodelivery systems explored include nanocomposite hydrogels, nanoparticles, nanoemulsion etc. A number of herbal and synthetic drugs examples of which include trichlosan, tetracycline, Harungana madagascariensis leaf extract, minocycline, metronidazole, chlorhexidine have been encapsulated into nanodelivery systems for treating periodontitis. A few examples of polymers investigated as matrices for the delivery of drugs to the periodontal pocket include chitosan, Poly lactic-co-glycolic acid copolymer, poly e caprolactone, polylactic acid, polypropylene, cellulose acetate propionate and ethyl vinyl acetate. In the near future also nanotechnology is expected to find its application in all the specializations of dentistry ranging from diagnosis and treatment of oral cancers to development of colloidal suspension containing millions of active analgesic micron-size dental robots resulting in anesthesia in patients. In the light of the above facts the current editorial focuses on the applications of nanotechnology based nanomedicines which cannot be undermined in the improvement of dental health and hygiene both, in the current as well as in future scenario.