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Intranasal nanostructured lipid carrier (NLC) of lurasidone hydrochloride (LRD) for brain delivery was prepared by the solvent evaporation method. The effects of independent variables, X1-lipid concentration, X-2 surfactant, and X-3 sonication times on dependent variables, Y1-particle size, Y-2 polydispersity index, and Y-3% entrapment efficiency were determined using Box-Behnken design. Optimized LRD-NLC was selected from the Box-Behnken design and evaluated for their morphological, physiological, nasal diffusion, and in vivo distribution in the brain after intranasal administration. Particle size, polydispersity index, and entrapment efficiency of optimized LRD-NLC were found to be 207.4 ± 1.5 nm, 0.392 ± 0.15, and 92.12 ± 1.0%, respectively. Transmission electron microscopy and scanning electron microscopy was used to determine the particle size and surface morphology of LRD-NLC. The prepared LRD-NLC follows biphasic in vitro drug release. Prepared NLC showed a 2-fold increase in LRD concentration in the brain when compared with the drug solution following intranasal administration. Results showed that intranasal route can be a good and efficient approach for delivering the drug directly to the brain and enhancing the drug efficacy in the brain for the management of schizophrenia and a good alternative to oral drug delivery.

The drug delivery across the brain has always been problematic due to the tight junction present namely the blood brain barrier (BBB). BBB only allows selected pharmaceutical drugs to get across it and reach the brain via lipid free diffusion process and exert their therapeutic effect. This leads to the decrease in drug accessibility to brain. More recently, various approaches were employed to allow larger molecules to cross BBB by reengineering them and conjugating them with ligands which could facilitate their entry across BBB. Therefore literature was explicitly exploited to deduce various ligands employed to enhance the drug delivery across brain via transcytosis. As per established literature, there are evidences that ligand conjugated drug formulations have substantially improved brain uptake. The review presents numerous ligands employed along with the receptor targeted to improve drug uptake by the brain, its anticipated effects and the outcome derived.

The present research work involves Quality by Design (QbD)-based fabrication of lipid nanoconstructs (LNC) of paliperidone (PPD) bearing superior biopharmaceutical attributes.LNC of paliperidone was prepared by melt emulsification-probe sonication and high-pressure homogenization method followed by optimization using QbD approach. Preparing LNC by both these methods will give the benefit of identifying the best optimized formulation which will be further evaluated for in vitro studies.The best optimized formulation was obtained using melt emulsification-probe sonication technique with small particle size (86.35 nm), high entrapment efficiency (90.07 %), and high loading capacity (8.49 %). The drug release from LNC was found to be 5, 8, and 9-folds greater than drug suspension in pH 1.2, 6.8, and 7.4 respectively (p0.001). Stability studies of LNC in simulated gastric fluid pH 1.2 and fasted state simulated intestinal fluid depicted no alteration in particle size and polydispersity index of LNC but were found to increase in fed state simulated intestinal fluid. The drug permeability through rat intestine for LNC was found to be approximately 6-folds (p0.05) greater as compared to the drug suspension which was further confirmed by confocal microscopy. The in vitro lipolysis study presented significantly highest solubilization (p0.001) in the aqueous phase thereby anticipating higher in vivo absorption.Thus, it was concluded that LNC bears the knack of improving the solubilization and permeation potential of an otherwise hydrophobic drug, paliperidone."

The treatment of acne warrants development of formulation aiming to enhance topical delivery with minimum systemic absorption. The aim of present study was to develop, optimize and characterize clindamycin phosphate-loaded nanostructured lipid carriers (CP-NLC) gel for enhanced topical delivery. CP-NLC was prepared using melt emulsification comibined with sonication technique using oleic acid (liquid lipid), precirol ATO5 (solid lipid), and tween 80 (surfactant). The optimized formulation attained using Box-Behnken statistical design exhibited particle size of 136 ± 0.11 nm, narrow PDI (0.256 ± 0.10), and high entrapment efficiency and high drug loading. TEM and SEM studies confirmed the spherical nature of the particles. Further, CP-NLC was loaded into Carbopol®940 gel and 1% concentration was evaluated for in vitro studies. The drug release from CP-NLC gel was 1.5-fold greater than from marketed formulation Clindac A®. The cumulative drug permeated through the skin was also found to be higher for CP-NLC gel (1.6-fold) than Clindac A® gel. The skin retention study, tape stripping technique and confocal laser scanning microscopy demonstrated enhanced skin retention and depth of permeation for CP-NLC gel. Therefore, formulating NLC for topical delivery of CP will render many benefits over marketed formulation thus proving as a promising carrier in the treatment of acne.