Carbamazepine and levetiracetam-loaded PLGA nanoparticles prepared by nanoprecipitation method: in vitro and in vivo studies


Kandilli B., UĞUR KAPLAN A. B., ÇETİN M., TAŞPINAR N., ERTUĞRUL M. S., AYDIN A. C., ...Daha Fazla

Drug Development and Industrial Pharmacy, cilt.46, sa.7, ss.1063-1072, 2020 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 46 Sayı: 7
  • Basım Tarihi: 2020
  • Doi Numarası: 10.1080/03639045.2020.1769127
  • Dergi Adı: Drug Development and Industrial Pharmacy
  • Derginin Tarandığı İndeksler: 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
  • Sayfa Sayıları: ss.1063-1072
  • Anahtar Kelimeler: Carbamazepine, epilepsy, levetiracetam, nanoparticles, PLGA
  • Uşak Üniversitesi Adresli: Evet

Özet

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 to in vitro characterize 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 and in vitro and in vivo characterized. Also, the antiepileptic effect of the NPs was evaluated in vivo in 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.