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Polymeric nanoencapsulation of zaleplon into PLGA nanoparticles for enhanced pharmacokinetics and pharmacological activity.
Haggag, Yusuf A; Abosalha, Ahmed Kh; Tambuwala, Murtaza M; Osman, Enass Y; El-Gizawy, Sanaa A; Essa, Ebtessam A; Donia, Ahmed A.
Afiliación
  • Haggag YA; Department of Pharmaceutical Technology, Tanta University, Tanta, Egypt.
  • Abosalha AK; Department of Pharmaceutical Technology, Tanta University, Tanta, Egypt.
  • Tambuwala MM; School of Pharmacy and Pharmaceutical Sciences, Ulster University, Coleraine, UK.
  • Osman EY; Department of Pharmacology and Toxicology, Tanta University, Tanta, Egypt.
  • El-Gizawy SA; Department of Pharmaceutical Technology, Tanta University, Tanta, Egypt.
  • Essa EA; Department of Pharmaceutical Technology, Tanta University, Tanta, Egypt.
  • Donia AA; Department of Pharmaceutical Technology, Menoufia University, Menoufia, Egypt.
Biopharm Drug Dispos ; 42(1): 12-23, 2021 Jan.
Article en En | MEDLINE | ID: mdl-33320969
Zaleplon (ZP) is a sedative and hypnotic drug used for the treatment of insomnia. Despite its potent anticonvulsant activity, ZP is not commonly used for the treatment of convulsion since ZP is characterized by its low oral bioavailability as a result of poor solubility and extensive liver metabolism. The following study aimed to formulate specifically controlled release nano-vehicles for oral and parenteral delivery of ZP to enhance its oral bioavailability and biological activity. A modified single emulsification-solvent evaporation method of sonication force was adopted to optimize the inclusion of ZP into biodegradable nanoparticles (NPs) using poly (dl-lactic-co-glycolic acid) (PLGA). The impacts of various formulation variables on the physicochemical characteristics of the ZP-PLGA-NPs and drug release profiles were investigated. Pharmacokinetics and pharmacological activity of ZP-PLGA-NPs were studied using experimental animals and were compared with generic ZP tablets. Assessment of gamma-aminobutyric acid (GABA) level in plasma after oral administration was conducted using enzyme-linked immunosorbent assay. The maximal electroshock-induced seizures model evaluated anticonvulsant activity after the parenteral administration of ZP-loaded NPs. The prepared ZP-PLGA NPs were negatively charged spherical particles with an average size of 120-300 nm. Optimized ZP-PLGA NPs showed higher plasma GABA levels, longer sedative, hypnotic effects, and a 3.42-fold augmentation in oral drug bioavailability in comparison to ZP-marketed products. Moreover, parenteral administration of ZP-NPs showed higher anticonvulsant activity compared to free drug. Oral administration of ZP-PLGA NPs achieved a significant improvement in the drug bioavailability, and parenteral administration showed a pronounced anticonvulsant activity.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Nanopartículas / Copolímero de Ácido Poliláctico-Ácido Poliglicólico / Acetamidas / Anticonvulsivantes Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Biopharm Drug Dispos Año: 2021 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Nanopartículas / Copolímero de Ácido Poliláctico-Ácido Poliglicólico / Acetamidas / Anticonvulsivantes Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Biopharm Drug Dispos Año: 2021 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Reino Unido