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Oral sorafenib-loaded microemulsion for breast cancer: evidences from the in-vitro evaluations and pharmacokinetic studies.
Chaurawal, Nishtha; Misra, Charu; Abul Barkat, Harshita; Jatyan, Reena; Chitkara, Deepak; Barkat, Md Abul; Sharma, Teenu; Singh, Bhupinder; Raza, Kaisar.
Afiliação
  • Chaurawal N; Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan, 305817, India.
  • Misra C; Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan, 305817, India.
  • Abul Barkat H; Department of Pharmaceutics, College of Pharmacy, University of Hafr Al-Batin, Al Jamiah, Hafr Al Batin, 39524, Saudi Arabia.
  • Jatyan R; Department of Pharmacy, Birla Institute of Technology and Science (BITS)-Pilani, Pilani Campus, Pilani, Vidya Vihar, Rajasthan, 333031, India.
  • Chitkara D; Department of Pharmacy, Birla Institute of Technology and Science (BITS)-Pilani, Pilani Campus, Pilani, Vidya Vihar, Rajasthan, 333031, India.
  • Barkat MA; Department of Pharmaceutics, College of Pharmacy, University of Hafr Al-Batin, Al Jamiah, Hafr Al Batin, 39524, Saudi Arabia.
  • Sharma T; University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India.
  • Singh B; Department of Pharmacy, Chandigarh College of Pharmacy, Landran, Punjab, 140307, India.
  • Raza K; University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India.
Sci Rep ; 12(1): 13746, 2022 08 12.
Article em En | MEDLINE | ID: mdl-35962160
Sorafenib tosylate (SFB) is a multikinase inhibitor that inhibits tumour growth and proliferation for the management of breast cancer but is also associated with issues like toxicity and drug resistance. Also, being a biopharmaceutical class II (BCS II) drug, its oral bioavailability is the other challenge. Henceforth, this report intended to encapsulate SFB into a biocompatible carrier with biodegradable components, i.e., phospholipid. The microemulsion of the SFB was prepared and characterized for the surface charge, morphology, micromeritics and drug release studies. The cell viability assay was performed on 4T1 cell lines and inferred that the IC50 value of sorafenib-loaded microemulsion (SFB-loaded ME) was enhanced compared to the naïve SFB at the concentrations of about 0.75 µM. More drug was available for the pharmacological response, as the protein binding was notably decreased, and the drug from the developed carriers was released in a controlled manner. Furthermore, the pharmacokinetic studies established that the developed nanocarrier was suitable for the oral administration of a drug by substantially enhancing the bioavailability of the drug to that of the free SFB. The results bring forth the preliminary evidence for the future scope of SFB as a successful therapeutic entity in its nano-form for effective and safer cancer chemotherapy via the oral route.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Nanopartículas Limite: Female / Humans Idioma: En Revista: Sci Rep Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Índia

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Nanopartículas Limite: Female / Humans Idioma: En Revista: Sci Rep Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Índia