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Tapentadol hydrochloride (TPD) is a novel analgesic with two mechanisms of actions: agonist activity at the μ-opioid receptor and norepinephrine reuptake inhibition. The conventional delivery of TPD is problematic, owing to its extensive first pass metabolism, low lipophilicity and short half-life that leads to low bioavailability (32%). The intent of the present work was aimed at bio-fabrication of polysorbate 80 coated chitosan nanoparticles (CS-NPs) for CNS targeting of TPD using factorial design approach for enhanced delivery of drug. TPD–CS-NPs were prepared by ionic gelation technique and optimized using 23factorial design of experiment. The effect of polymer (CS) and cross linker (TPP) concentration was studied on particle size (PS) and entrapment efficiency (EE%). Formulation CNP6was considered desirable with optimalEE% (87.1 ± 0.4%),PS(329.3 ± 1.0 nm), zeta potential (30.4 ± 0.7 mV) and cumulative drug release of 73.5 ± 2.9% in 24 h. Differential scanning calorimetry revealed the absence of any chemical interaction between TPD, CS, and TPP while SEM study confirmed spherical morphology.In vivopharmacodynamic studies on rat model verified that pure drug was unable to show considerable antinociceptive activity owing to its hydrophilic nature, conversely polysorbate 80 coated TPD–CS-NPs showed a significant antinociceptive effect over a period of 24 h, which is evidence for brain targeting of TPD–CS-NPs. Accelerated stability studies of optimized batch demonstrated a negligible change in the averagePSandEE% after storage at 25 ± 2 °C/60 ± 5% RH (relative humidity) for the period of three months. The ANOVA results for the dependent variables demonstrated that the model was significant (Pvalues < 0.05) for response variables. Above finding suggested practicability of investigated system for effective targeting of many therapeutic agents in the treatment of many life threatening CNS disorders. [ABSTRACT FROM AUTHOR]

Present invention relates to design of nanostructured lipid carriers (NLC) to augment oral bioavailability of Carvedilol (CAR). In this attempt, formulations of CAR-NLCs were prepared with glyceryl-monostearate (GMS) as a lipid, poloxamer 188 as a surfactant and tween 80 as a co-surfactant using high pressure homogenizer by 23factorial design approach. Formed CAR-NLCs were assessed for various performance parameters. Accelerated stability studies demonstrated negligible change in particle size and entrapment efficiency, after storage at specified time up to 3 months. The promising findings in this investigation suggest the practicability of these systems for enhancement of bioavailability of drugs like CAR. [ABSTRACT FROM PUBLISHER]

We report the development of Layer-by-Layer (LbL) polyelectrolyte self-assembled nanocrystalline drug-delivery platform using two experimental factors, namely the number of coatings and temperature during deposition with three varying levels. The optimized formulation (Fopt) was assessed for zeta potential and particle size using Fourier Transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), and Scanning Electron Microscopy (SEM). Charge reversal along with an increase in particle size confirmed coating of polyelectrolyte on drug nanocrystals. The FT-IR study revealed no signs of incompatibility or change in formulation property during preformulation and stability study. This fact was further supported by DSC results. [ABSTRACT FROM PUBLISHER]