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The study's purpose intended to develop and optimize an NLC formulation for topical berberine administration with increased skin acne efficacy. The “three-parameters, three-level Box-Behnken design” was employed to improve the formulation based on vesicle size, PDI, and encapsulation efficiency. In-vitro profile for drug release, skin penetration investigation using confocal microscopy, skin irritation, anti-inflammatory, and anti-acne studies were performed on the optimized formulation. The vesicles with a size of 132.5 ± 10.34 nm, PDI of 0.224 ± 5.12, and entrapment efficiency of 85.956 ± 5.78% were found in the optimized formulation. The optimized formulation had spherical vesicles, according to TEM imaging. In vitro release studies showed that final optimized NLC formulation has cumulative release of drug (72.675 ± 3.686%), which was significantly greater as compared to NLC gel formulation (48.354 ± 4.893%). Thermo-analytical studies of NLCs formulation determined smooth drug interaction via rat skin membrane. Confocal microscopy revealed that, rhodamine-NLC formulation was traceable up to 54.9 μm across skin of rats, while solution of rhodamine penetrated only up to 20.4 μm of rat skin. Skin irritation study further showed significantly lower irritation level of skin (erythema: 0.50.231 and edema: 0.50.320) by applying optimized NLC-gel formulation compared to the control irritant. Furthermore, in comparison to the positive control, the anti-acne study demonstrated a decrease in all acne parameters, in addition to higher effectiveness over the commercially available formulation. These findings suggest that developed berberine loaded NLC gel could be a promising vehicle for the safe and effective topical administration of drugs to treat acne vulgaris.

Thymoquinone (TQ) is a potent phytoconstituent from Nigella sativa and well recognized for its neuroactivity via antioxidant mechanisms, but its higher lipophilicity and plasma protein binding lowers its bioavailability negating any appreciable clinical outcome, thus losing the possibility to form any conventional dosage form. TQ's brain targeted drug delivery can result into an increased efficacy and bioavailability, thus, in a novel attempt, we aim to formulate brain targeted Polysorbate-80 coated thymoquinone PLGA nanoparticles (P-80-TQN) and evaluate their activity towards Alzheimer's disease. The modified single-emulsion solvent-evaporation technique was employed to formulate the TQN and further coated by Polysorbate-80 to obtain brain targeted P-80-TQN. The effectiveness of TQ released from P-80-TQN was evaluated in Alzheimer's (AD), biochemically by Super-Oxide Dismutase (SOD) enzymatic assay and behaviorally by Despair Test in Streptozotocin-(STZ)-induced Alzheimer's mice models at 5 mg/kg TQ-equivalent dose. AD markers: β-amyloid tangles were validated through histopathology of the brain's hippocampal tissues from euthanized mice. A Stable and homogenous targeted P-80-TQN (226.2 nm, ζ = −45.6 mV) formulation was prepared and characterized physiochemically and spectrally. It significantly reduced the IT (39.45 ± 3.32 s), and increased SOD functioning (8.33 ± 2.61 units/mg) after treating mice for 28 days at 5 mg/kg equivalent P-80-TQN. An invitro biphasic cumulative release of TQ (59.10 ± 2.10) from P-80-TQN was observed over 24 h, whereas invivo TQ release in brain from P-80-TQN was observed and explained in terms of AUC (0–600mins) and Cmax which were obtained 4.5 and 4.3 times respectively and Tmax was 3 times faster than normal TQ. A reduced and solvated protein aggregates (

Topical ocular delivery of therapeutics are always a challenging arena in order to achieve high ocular bioavailability with safe administration. Ideal ocular delivery of drug required 4 P's that is Patient compliance, Prolong retention, Penetration to cornea and Prolong release of drug. In an attempt to achieve desired characteristics for ocular delivery, Ketorolac loaded PLGA nanoparticles were fabricated by double emulsification solvent evaporation method and optimized by employing response surface methodology (RSM) followed by statistical analysis. Results obtained by RSM were further validated for fitness in model by different checkpoint formulations. Vitamin E TPGS was selected as emulsifier, which acquires high emulsifying capability and high permeability character. Zeta-size study revealed that optimized formulation has mean particle size 142.8 ± 11.7 nm, which was in agreement of TEM study and zeta potential was found −24.2 ± 1.2 mV. Encapsulation efficiency was achieved 63.5 ± 8.4%. Release profile was established by different mathematical modelling. It was observed that optimized formulation showed sustained release and followed by Korsmeyer-Peppas model. Corneal transport study showed enhanced drug permeation as compared to drug solution. HET-CAM test and histopathology studies revealed that optimized PLGA NPs was non-irritant and safe for ocular application.

In the present study, we selected two potential herbal drugs (Smilax china and Salix alba) and developed nano lipidic carriers (NLC) gel for safe and effective topical therapy against psoriasis. Optimization of formulation of NLCs was performed using Box-Behnken design by selecting three input variables viz. lipid concentration, surfactant concentration and sonication time at three levels; and evaluated for the average particle size, polydispersity and %encapsulation as the response parameters. The outcomes of the present study showed that optimized dual drug-loaded NLCs had low average particle size (150.20 ± 3.57 nm) and polydispersity (0.301 ± 0.01) and high entrapment (86.32 ± 2.78% w/w). TEM imaging of the optimized formulation showed spherical vesicles. The drug release and dermal transport studies revealed sustained drug release (57.55 ± 5.38%) and enhanced dermal flux (3.88 μg/cm2/h), respectively. Thermo-analytical studies of NLCs showed fluidized state of the membrane of mice skin for smooth penetration of drugs. Confocal study revealed uniform distribution and deeper layer penetration of the optimized NLC gel system as compared to hydroalcoholic solution. Further, dermatokinetic study showed improved penetration of drug-loaded NLC gel in mice skin than the marketed formulation. The score obtained from skin irritation study revealed non-irritancy of the developed system. Further, in the developed psoriatic model, PASI score established decline in all the parameters as compared to the toxic control group, as well as better efficacy than the marketed formulation. Hence, the obtained results construe that developed NLCs as potential carriers for the effective and safe topical delivery of herbal drugs.