The present investigation demonstrated enhanced delivery of asiatic acid using glutathione and hence served as a potential ligand to improve brain targeting efficiency.
Bergenia ciliata (Haw) Sternb. possess immunomodulatory, anti-inflammatory, antioxidant, anti-urolithiatic, wound healing, anti-malarial, anti-diabetic and anti-cancer properties. Moreover, the methanolic extracts of the rhizomes of the plant were found to demonstrate beneficial neuroprotective effects in the intracerebroventricular streptozotocin-induced model in rats. Thus, the present study was undertaken to further explore the neuroprotective potential of the aqueous (BA) and methanolic extracts (BM) of B. ciliata through various in-vitro and in-vivo studies. Both the extracts at all tested concentrations i.e. 50-50,000 ng/mL did not cause any significant reduction of cell viability of SH-SY5Y cells when tested for 48 h when assessed through MTT and resazurin metabolism- based cell viability assays. The pre-treatment with the extracts could confer significant (p < 0.001) and dose-dependent protective effects against NMDA induced injury in SH-SY5Y cells. BM [IC: 5.7 and 5.19 μg/mL for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) respectively] led to more potent inhibition of both the enzymes as compared to BA (IC: 227.12 and 23.25 μg/mL for AChE and BuChE respectively). BM also proved to be a 1.85-fold better scavenger of the DPPH free radicals as compared to BA. Thus, BM was taken further for the evaluation of the beneficial effects of 14-day pre-treatment in rats in the scopolamine (2 mg/kg, i.p.) induced amnesia model at 125, 250 and 500 mg/kg, p.o. BM pre-treatment at 250 and 500 mg/kg could significantly ameliorate the cognitive impairment (p < 0.001), inhibit AChE (p < 0.001) and BuChE (p < 0.05) activity, restore GSH levels (p < 0.05) in serum and brain homogenates and recover the morphology of hippocampal neurons back to normal. Moreover, the BM administration at 500 mg/kg also showed beneficial effects through the significant (p < 0.05) reduction of Aβ, phosphorylated tau (p-tau) and GSK-3β immunoreactivity in the brain homogenates of the intracerebroventricularly streptozotocin (ICV STZ) injected rats as observed from the results of the ELISA assays. The outcomes of the study unveiled that BM exerts its beneficial effects through prevention of NMDA induced excitotoxic cell death, dual cholinesterase inhibition, antioxidant activity coupled with the reduction of the immunoreactivity for the Aβ, p-tau and GSK-3β indicating its potential to be screened further for various other models to determine the exact mechanism of action.
To cite this article: Nisith Raval, Priyal Barai, Niyati Acharya & Sanjeev Acharya (2018) Fabrication of peptide-linked albumin nanoconstructs for receptor-mediated delivery of asiatic acid to the brain as a preventive measure in cognitive impairment: optimization, in-vitro and invivo evaluation, Artificial Cells, Nanomedicine, and Biotechnology, 46:sup3, S832-S846,
ABSTRACTThe aim of the study was to evaluate the neuroprotective activity of glutathione (GU)-conjugated asiatic acid (AA) loaded albumin nanoparticles and establishing the drug targeting efficiency (DTE) of GU as a selective ligand for brain-targeted delivery. Albumin nanoparticles were prepared by desolvation technique and optimized using quality by design (QbD) approach. GU was conjugated with nanoparticles by carbodiimide reaction and characterized by its size and zeta potential using dynamic light scattering phenomenon. Dialysis bag technique was employed for in-vitro release study and in-vivo brain targeting efficiency was evaluated in Sprague-Dawley rats (75 mg/kg, i.p.). Neuroprotective activity was evaluated against scopolamine-induced dementia in rats. Resultant brain bioavailability of nanoparticles with 100.2 nm size and 71.59% entrapment efficiency (EE), was found 7-fold higher than AA dispersion with 293% DTE for the brain. Conjugated nanoparticles showed significantly high percentage correct alternation (p < .05), low escape latency time (p < .01), cholinesterase inhibition (p < .01) and ameliorated GU levels (p < .01) as compared to diseased animals. GU showed potential to enhance the brain delivery of AA with ameliorated neuroprotective activity due to enhanced bioavailability. This concept can serve as a platform technology for similar potential neurotherapeutics, whose clinical efficacy is still challenging owing to poor bioavailability.
ARTICLE HISTORY
Abstract:Sun is the continuous source of renewable energy, from where we can get abundant of solar energy. Concept of conversion of solar energy into heat was used back in 200 B.C. since then, the solar cells have been developed which can convert solar energy into the electrical energy and these systems have been produced commercially. The technologies to enhance the power conversion efficiency (PCE) have been continuously improved. Different technologies used for developing solar cells can be categorized either on the basis of material used or techniques of technology development which is further termed as 'first generation' (e.g. crystalline silicon), 'second generation' (thin films of Amorphous silicon, Copper indium gallium selenide, Cadmium telluride), 'Third generation' (Concentrated, Organic and Dye sensitize solar cell). These technologies give PCE up to 25% depending on the technology and the materials used. Nanotechnology enables the use of nanomaterial whose size is below 100 nm with extraordinary properties which has the capability to enhance the PCE to greater extent. Various nanomaterials like quantum dots, quantum well, carbon nanotubes, nanowire and graphene have been used to make efficient and economical solar cells, which not only provide high conversion efficiency economically but also are easy to produce. Today, by using nanotechnology, conversion efficiency up to 44.7 % has been achieved by Fraunhofer Institute at Germany. In this review article, we have reviewed the literature including various patents and publications, summarized the history of solar cell development, development of different technologies and rationale of their development highlighting the advantages and challenges involved in their development for commercial purpose. We have also included the recent developments in solar cell research where different nanomaterials have been designed and used successfully to prove their superiority over conventional systems.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.