Development, characterization and cytotoxicity evaluation of Gingko biloba extract (EGB761) loaded microemulsion for intra-nasal application

Abstract

Background: Ginkgo biloba is therapeutically important fossil species with extended benefits against CNS disorders as; it contains various potential constituents which are known for their specific actions. In spite of this fact its medicinal usage are limited due to the limited absorption, rapid elimination, vigorous biotransformation and low bioavailability of its therapeutic components. Objective: The present study is an attempt to develop a microemulsion system of standardized extract of Ginkgo biloba (EGB761) for intranasal application. Material and methods: It is developed by water titration method using Isopropyl Myristate (oil), Tween 80 (surfactant) and Ethanol (co surfactant). Results: EGB761 loaded microemulsions were developed and characterized. The optimized formulation showed particle size of 259.8 ± 6.3 nm, PDI score of 0.186 ± 0.092 and zeta potential as -9.87 ± 2.23 mv. Also, TEM images showed size range from 84 -260 nm with smooth and spherical morphology. In vitro phyto-constituents release through isolated nasal mucosa showed release pattern of zero order kinetics with sustained release (up to 16 hours). Moreover, cytotoxicity evaluation (RPMI2650 cell lines) didn't show cytotoxicity for both GBME (99.3 % ± 2.28 % and 98.17 % ± 1.86%) and plain EGB761 extract (95.3 % ± 2.1 and 91.7 % ± 1.07) with different time periods (3 and 12 hours). Conclusion: Therefore, it has been concluded from the results that, EGB761 based microemulsion (GBME) is developed with particle size range between 84 -260 nm, having zero order release kinetics. GBME is found to be safe on RPMI2650 cell line and can be further, investigated in in vivo system.

Bio Pharmaceutics Classification System (BCS) Class IV Drug Nanoparticles: Quantum Leap to Improve Their Therapeutic Index

“…Fourier Transform Infrared Spectroscopy (IR-810, JASCO, Tokyo) was done to identify the functional groups present and interaction between the core molecules of HCTZ and outer polymeric shell. For analysis, the test samples were prepared by potassium bromide disc method 17 and FT-IR spectra of HCTZ, optimized nanocoacervates without HCTZ and with HCTZ were scanned from 400-4000 cm -1 band width.…”

Untitled

“…The stability testing of TTO and TTO-ME was performed by the method as reported by Singh et al, 2017. [45] Since the retention of the essential terpenoid group of TTO was important for maintaining the therapeutic efficacy of the formulation; hence, the optimized formulation (TTO-ME) was tested initially after formulation and then after storing it at room temperature (37°C) for 1 year by terpenoid estimating assay as discussed above. [46] In this assay, the stability of TTO and TTO-ME at variable concentrations (100-1000 µl/ml) was tested and compared it with its terpenoid content.…”

Antioxidant, Cytotoxicity, and Stability Evaluation of Ginkgo Biloba Extract-Based Microemulsions for Enhanced Therapeutic Activity

“…Standardized extract of G. biloba, has higher content of potential compounds such as flavonoids, polyphenols, and terpenoids, but these compounds are not very stable and get degraded easily in gut and other tissue fluids and also have shorter shelf life [17]. There are various other factors which lead to their low bioavailability, bioefficacy, permeability, and poor stability [18].…”