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The aim of the presented study was to develop PEGylated liposomes of Temozolomide (TMZ) that provide optimum drug concentration at tumor site. Reverse phase evaporation (REV) method was used to prepare TMZ-loaded PEGylated liposomes. Formulation was optimized by using design expert software by 3 factorial design. The physicochemical properties including size, morphology, entrapment efficiency, drug loading, etc. of formulated liposomes were evaluated. Finally, the optimized formulation was selected for in vitro drug release and stability study. In vivo pharmacokinetic study in rats showed that TMZ-loaded PEGylated liposomes leads to 1.6-fold increase in AUC in blood and 4.2-fold increase in brain as compared to free drug solution. This formulated PEGylated liposomes offers a promising approach for treatment of Glioblastoma Multiforme.

Aim: The manuscript describes the performance of nanoparticles loaded with antidepressant drug for nose-to-brain drug delivery. Materials & methods: Poly-lactic-co-glycolic acid-loaded nanoparticles of agomelatine were prepared by nanoprecipitation method using poloxamer 407 as stabilizer. The process parameters were optimized using factorial design. Results: The drug-loaded nanoparticles having low particle size (<200 nm) with narrow size distribution and required zeta potential (-22.7 mV) to avoid aggregation showed sustained release profile and were found to have higher permeability as observed from ex vivo studies when compared with plain drug suspension. Histopathology test showed that the optimized formulation was free from nasal toxicity on the goat nasal mucosa. Pharmacodynamic study showed significant reduction in immobility time in rats treated with the formulation which indicated antidepressant activity of the formulation. Conclusion: The prepared agomelatin-loaded poly-lactic-co-glycolic acid nanoparticles showed prominent antidepressant activity by nose-to-brain delivery as observed from various studies.

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Aim: The work describes enhanced bioavailability of paliperidone palmitate through transdermal delivery using nanostructured lipid carriers (NLC). Materials & methods: NLCs were formulated by nanoprecipitation method followed by incorporation in transdermal patch and physicochemical characterization. Results: NLCs showed high percentage entrapment efficiency of 83.44 ± 0.8%, drug loading of 24.75 ± 1.10% (w/w), particle size of 173.8 ± 3.25 nm, polydispersity index of 0.143 ± 0.05 and zeta potential of -15.9 ± 0.75 mV. In vitro and ex vivo studies indicated zero-order controlled drug release from NLCs and transdermal patch up to 48 h. Pharmacokinetic studies indicated 1.76-fold enhanced bioavailability by transdermal route as compared with oral drug delivery. Conclusion: From the results, it was concluded that drug-loaded NLCs-transdermal patch is promising drug delivery system for poorly bioavailable drugs.