Carbamazepine and levetiracetam-loaded PLGA nanoparticles prepared by nanoprecipitation method:in vitroandin vivostudies


Kandilli B., Ugur K., Cetin M., Taspinar N., Ertugrul M., Aydin İ. Ç. , ...More

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, vol.46, no.7, pp.1063-1072, 2020 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 46 Issue: 7
  • Publication Date: 2020
  • Doi Number: 10.1080/03639045.2020.1769127
  • Journal Name: DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Biotechnology Research Abstracts, Business Source Elite, Business Source Premier, CAB Abstracts, Chemical Abstracts Core, EMBASE, International Pharmaceutical Abstracts, MEDLINE, Veterinary Science Database
  • Page Numbers: pp.1063-1072
  • Keywords: Carbamazepine, epilepsy, levetiracetam, nanoparticles, PLGA, SEIZURE MODEL, COMBINATION THERAPY, ANTIEPILEPTIC DRUGS, EPILEPSY TREATMENT, ACID, DELIVERY, TOPIRAMATE, COPOLYMER, TOXICITY, RELEASE
  • Erzincan Binali Yildirim University Affiliated: No

Abstract

Objective:The aim of this study was to develop the PLGA nanoparticles (NPs) containing carbamazepine (CBZ) and levetiracetam (LEV) combination (CBZ + LEV) for the treatment of epilepsy and toin vitrocharacterize the prepared NPs. Significance:LEV and CBZ, which are antiepileptic drugs, are used in the treatment of epilepsy. Nano-sized formulations are prepared to use for different purposes such as to improve the solubility/the physicochemical properties and bioavailability of drugs, to decrease their doses and frequency of administration, and to reduce side effects of drugs. Methods:CBZ + LEV-PLGA-NPs were prepared by a modified nanoprecipitation method andin vitroandin vivocharacterized. Also, the antiepileptic effect of the NPs was evaluatedin vivoin a rat epilepsy model. Results:The mean particle size and zeta potential of CBZ + LEV-PLGA-NPs were 180.62 +/- 6.260 nm and -27.08 +/- 3.110 mV, respectively. The values of encapsulation efficiency (EE%) of CBZ and LEV were 51.00 +/- 5.944% and 2.05 +/- 0.367%, respectively. CBZ showed a biphasic release profile with initial burst release followed by a sustained release. Ninety percent of CBZ was released from NPs within two days; however, % LEV release from NPs reached about 80% within 30 min. Conclusion:Our results showed that a decrease in seizure scores in the group treated with CBZ + LEV was observed and also, CBZ + LEV and CBZ + LEV-PLGA-NPs had similar antiepileptic activity. The NPs containing CBZ + LEV might be beneficial in the treatment of epilepsy.