Aim: The aim of the present study was to develop and optimize the self-nanoemulsifying drug delivery system of α-pinene (ALP-SNEDDS) and to evaluate its in-vivo anti-Parkinson’s activity. Background: Different lipid-based drug delivery technologies have been researched to upgrade the bioavailability of such drug candidates and to expand their clinical adequacy upon oral administration. Self-emulsifying drug delivery system (SEDDS) have pulled in expanding interests and, specifically, self-nanoemulsifying drug delivery system (SNEDDS). Objective: The present work was an attempt in order to improve the bioavailability of the ALP via defining the role of self-nanoemulsifying formulations for its neuroprotective effect. Method: Miscibility of the ALP was estimated in various excipient components to select the optimized combination. Self-nanoemulsification, thermodynamic stability, effect of dilution on robustness, optical clarity, viscosity and conductivity tests were performed. The in-vivo anti-Parkinson’s activity of the ALP-SNEEDS formulations were done by using Pilocarpine antagonism induced Parkinsonism in rodents. Behavioural tests like tremulous jaw movements, body temperature, salivation and lacrimation are performed. Result: Two optimized formulation, composed of Anise oil, Tween 80 and Transcutol-HP of Oil: Smix ratio (4:6 and 3:7) were selected. The Smix ratio for both the formulation was 2:1. The particle size was found to consistent with the increase in dilution. The mean negative zeta potential of the formulations was found to be increased with increase in dilution. The TEM images of the formulations reveals spherical shape of the droplet. The in-vitro drug release profile was found to be significant as compared to plain ALP suspension. Conclusion: The results form in-vivo studies indicate that nanosizing and enhanced solubilisation of oral ALP-SNEDDS formulations significantly improved the behavioural activities as compared to plain ALP suspension.

Objective: The motivation behind the current examination was to build the solvency and dissolution rate of an antihypertensive drug telmisartan by the planning of nanosuspension by precipitation method at the research facility scale. We researched the nanoparticle manufacture of telmisartan employing a 33 factorial experimental configuration considering the impacts of nanosuspension on the physical, morphological, and dissolution properties of telmisartan. Methods: To get ready, nanosuspension particles of an ineffectively dissolvable drug are moreover of a drug solution to the anti-solvent leads to abrupt supersaturation and precipitation the making of nanoparticles. The nanosuspension particles of a poorly soluble drug loaded with urea and surfactants (sodium lauryl sulfate (SLS), poloxamer 188, Tween 80) have been prepared by a precipitation method. The nanosuspension particles were characterized for particle size, zeta potential, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), in vitro drug release, and release kinetics. Results: The readily optimized batch nanosuspension particles evaluated and exhibited the particle size (750 nm), zeta potential (-24.33 mV), differential scanning calorimetry (DSC) drug exhibited a change in crystalline form to amorphous, in vitro dissolution (F12 was higher 95% within 5 min) and drug release kinetics. The formulation parameter of surfactant concentration is optimized. Conclusion: The formulation of the nanosuspension approach has been shown to substantial improvement in the dissolution rate, thereby enhancing the oral bioavailability with the future development of this technology.

Abstract:: Substantial affirmation suggested that oxidative stress remains an impelling target, contributing to initiate and exacerbate the multiple neurological complications in age-related neurodegeneration (ARN). Factors including gene and environmental toxins now becoming the most threatening cause of oxidative stress. It leads to mitochondrial dysfunction of the neurons that ultimately causes permanent loss of its functionality. Clinical trials on antioxidants are still in the pipeline to access it as a potential therapeutic class. But this raised the generosity for not only to investigate the module of the antioxidant mechanism but also to justify the drug delivery and doses regimen. Biological barriers predominantly Blood-brain barrier (BBB) and rapid first-pass metabolism are some of the potential obstacles for the effective targeting of the therapeutic agent. Bioactive drugs with antioxidant capacity, loaded with lipid-based Nano career system has revealed to be a novel therapeutic intervention for ARN. The review will deal with the comprehensive state-of-art methodology for the delivery of bioactive loaded lipid Nanocarriers to treat neurodegeneration. A systematic analysis of published reports will help the researchers to understand the role of natural compound loaded Nanoengineered system in the field of ARN as a potential Nano therapeutic intervention.

Aim: The present study was expected to explore the molecular interaction of five oxidative stress (OS) associated target receptors with Alpha-Pinene and its antioxidant validation for the effective treatment of Parkinson’s disease (PD). Background: Oxidative stress (OS) via multitudinous cascades is considered to be the leading attribute to dopaminergic cell degeneration in PD. Furthermore, it is also well-linked to other mechanisms involved in the neurodegeneration process, like dysfunction of mitochondria, neuroinflammation and excitotoxicity due to NO. Objective: The present investigation was to establish a molecular association of OS-associated target receptors with the bioactive compound alpha-pinene and how this molecular interaction empowers the mitigation of PD. Material and Method: Five different molecular targets namely Peroxisome Proliferator-Activated Receptor- Gamma (PPARγ), Liver-X receptor beta (LXR- β), Human Monoamine Oxidase-B (MAO-B), Human Nuclear receptor related-1 protein (Nurr1) and Human Lipoprotein-associated phospholipase A2 (Lp-PLA2) were obtained from RCSB-PDB, which has some leading association in the inhibition of the OS-induced neurodegeneration. Molecular interactions were stuffed by the simulation molecular docking software. Antioxidant activity was validated by in-vitro models as per standardized procedures against 2,2- diphenyl-1- picrylhydrazyl (DPPH), 2,2'-azinobis-(3-ethylbenzothiazoline -6-sulfonic acid) (ABTS), Ferric ion (Fe3+), Hydroxyl (•OH), nitric oxide (•NO), Peroxynitrite (ONOO-) and Hypochlorous acid (HOCl). Result: Our results indicated that alpha-pinene can interact with all the five different target receptors at the active binding site of receptors. Alpha-pinene was found to show better interaction with MAO-B, Nurr1 and PPARγ with binding energy of -5.50, -4.52 and -5.25, respectively as compared to the native ligand. Furthermore, the interaction of alpha-pinene with LXR-β and Lp-PLA2 was also significant with binding energy of -5.6 and -5.12, respectively. It also capable of neutralizing all the different free radicals under consideration with significant IC50 values against HOCl and •NO. Conclusion: It might be concluded that alpha-pinene could act as a potential inhibitor and scavenger of OS which could act on the multiple target receptors under consideration.

Aim: The aim of the present investigation was to develop a polyherbal nano gel (PHNG) formulation capable of acting as a potential vehicle to deliver polyherbal phytoconstituents topically. Background: Individual herbs, according to Ayurveda, are insufficient to deliver the intended medicinal effect. It will have a better therapeutic impact with less toxicity when it is optimized as multiple herb combinations in a certain ratio. Objective: The objective of this study was to create a polyherbal gel for the delivery of medication from methanolic extracts of Plumbago zeylanica Linn, Datura stramonium Linn, and Argemone mexicana Linn. Material and methods: this work include methanolic extracts of Plumbago zeylanica stem, Datura stramonium leaves, Argimone Mexicana areal part. The polyherbal-based nanogel was prepared by low energy self-emulsification technique, and was evaluated for pH, viscosity and spreadability, stability, and drug release. The drug release profile of stable nanogel formulations was studied at various time intervals. Furthermore, the prepared nanogel was characterized by zeta-potential, zeta-sizer, and transmission electron microscopy (TEM). Result: Optimized PHNG had particle size and zeta potential of 11.25nm and -25.73 mV respectively. TEM analysis of optimized formulation revealed the spherical shape of particles. Furthermore, the optimized formulation was found to possess higher stability with a maximum extended cumulative release of up to 240 minutes Conclusion: We have formulated a polyherbal nanogel that can be validated by physiochemical and surface characterization.