FORMULATION AND OPTIMIZATION OF NANOEMULSION DRUG DELIVERY SYSTEM CONTAINING PHENYTOIN FOR EPILEPSY TREATMENT

Epilepsy is a central nervous system (CNS) disease whereby abnormal electrical activity is present in the brain resulting in seizures. Epileptic patients are prescribed with anti-epileptic or anti-convulsant drugs. Various approaches have been explored to treat the disease. However, challenges of modern anti-epileptic drugs (AEDs) nowadays are the difficulty of the drugs to penetrate the blood brain barrier (BBB) which results in poor efficacy thus many patients develops resistance against AEDs. Nanoemulsions have been increasingly developed for use as drug delivery systems. It offers several significant advantages including powerful permeation ability with high drug-loading capacity, enhanced bioavailability and drug stability. In this project, formulation of nanoemulsion containing phenytoin (PHT), an anticonvulsant drug will be prepared using a mixture of both low and high energy emulsification techniques. The optimization of nanoemulsion will be carried out using response surface methodology (RSM) and mixture design (MD) techniques. The investigations of the physicochemical properties of nanoemulsion such as particle size, morphology and the stability of the droplet size will be evaluated. The efficacy of the PHT from nanoemulsion will be tested in-vivo and in-vitro through blood brain barrier (BBB). By doing these tests PHT-loaded nano-emulsions could be promising carriers having the potential to improve the drug bioavailability in brain tissue.

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Title : Characterisation, in-vitro and in-vivo evaluation of valproic acid-loaded nanoemulsion for improved brain bioavailability
Description :
This study was aimed to investigate the potential of formulated valproic acid-encapsulated nanoemulsion (VANE) to improve the brain bioavailability of valproic acid (VPA).
Authors : JOHNSON A/L STANSLAS
URL :
1) https://www.scopus.com/record/display.uri?eid=2-s2.0-85030646325&origin=resultslist&sort=plf-f&src=s&st1=stanslas&st2=&sid=0d70d1dbae08e52deaf65eb32c27ce87&sot=b&sdt=b&sl=21&s=AUTHOR-NAME%28stanslas%29&relpos=0&citeCnt=0&searchTerm=

Date Publish : 14/12/2017
Title : Development of Nanoemulsion containing Centella Asiatica Crude Extract as a Promising Drug Delivery System for Epilepsy Treatment
Description :
Preparations of products containing herbal extracts have grown by leaps and bounds, hitting the pharmaceutical industries due to the natural healing approach. Centella asiatica L. (pegaga) (C. asiatica) is a famous plant commonly served as a salad in Asian diets. It contains various phytoconstituents, which plays a vital role in the treatment of various illness. For example, in the treatment of epilepsy, crossing the blood-brain barrier (BBB) has been a challenge (even as parenteral application) as not all the drugs were able to pass through the membrane and produce a maximum therapeutic effect to the targeted site of action. Thus, a nanoemulsion formulation containing C. asiatica crude extract needs to be developed to penetrate the BBB. This study aims to formulate a nanoemulsion containing crude extract of C. asiatica leaves for epilepsy treatment. Nanoemulsion was prepared by using low energy emulsification method. The particle size, polydispersity index (PDI), and zeta potential of C. asiatica crude extract nanoemulsion were found to be at 57.86 ± 0.03 nm, 0.50 ± 0.03, and -26.50 ± 0.03 mV, respectively. The formulation remained physically stable at different storage temperatures (4, 25, and 45 °C) for 90 days. The particle size observed by transmission electron microscopy (TEM) was shown to be at ̴ 50 nm, which correlated well with the Zetasizer analysis. The cytotoxicity study, conducted on formulated C. asiatica nanoemulsion towards Vero cell line and 3T3 cell line, showed that the IC50 value indicated that it is nontoxic (>500 μg/ml). C. asiatica nanoemulsion was found to be stable based on the good evidence of physicochemical properties, and the IC50 value indicates significance for future in vivo and in vitro studies based upon the route of administration
Authors : HAMIDON BIN BASRI,NUR KARTINEE BINTI KASSIM,INTAN DIANA BINTI MAT AZMI
Date Publish : 17/06/2022
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