Ribociclib Nanostructured Lipid Carrier Aimed for Breast Cancer: Formulation Optimization, Attenuating In Vitro Specification, and In Vivo Scrutinization.

Purpose. The current investigation is on the explicit development and evaluation of nanostructured lipidic carriers (NLCs) through the oral route to overcome the inherent lacuna of chemotherapeutic drug, in which Ribociclib (RBO) was used for breast cancer to diminish the bioavailability issue. Meth...

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Publicado en:BioMed Research International pp. 1 - 25
Autores principales: Sartaj, Ali, Annu, Biswas, Largee, Verma, Anita Kamra, Sahoo, P. K., Baboota, Sanjula, Ali, Javed
Formato: equations & formulas pictorial research tables/charts Journal Article
Publicado: Wiley-Blackwell 2/3/2022
Acceso en línea:Ver este registro en EBSCOhost
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      dt: 2/3/2022
      pid: 480
      pub: Wiley-Blackwell
      place: Malden, Massachusetts
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        155059190
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        10.1155/2022/6009309
        155059190
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        atl: Ribociclib Nanostructured Lipid Carrier Aimed for Breast Cancer: Formulation Optimization, Attenuating In Vitro Specification, and In Vivo Scrutinization.
      aug:
        au:
          Sartaj, Ali
          Annu
          Biswas, Largee
          Verma, Anita Kamra
          Sahoo, P. K.
          Baboota, Sanjula
          Ali, Javed
        affil: Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India
      sug:
        subj:
          Antineoplastic Agents Therapeutic Use
          Nanostructures
          Drug Delivery Systems
          Breast Neoplasms Drug Therapy
          Chemistry, Pharmaceutical
          Biological Availability
          Human
          Female
          In Vitro Studies
          In Vivo Studies
          Treatment Outcomes
          Cancer Patients
          Female
      ab: Purpose. The current investigation is on the explicit development and evaluation of nanostructured lipidic carriers (NLCs) through the oral route to overcome the inherent lacuna of chemotherapeutic drug, in which Ribociclib (RBO) was used for breast cancer to diminish the bioavailability issue. Method. The RBO-NLCs were prepared using the solvent evaporation method and optimized method by the Box–Behnken design (BBD). Various assessment parameters characterized the optimized formulation and their in vivo study. Results. The prepared NLCs exhibited mean particle size of 114.23 ± 2.75 nm , mean polydispersity index of 0.649 ± 0.043 , and high entrapment efficiency of 87.7 ± 1.79 %. The structural analysis by TEM revealed the spherical size of NLCs and uniform drug distribution. An in vitro drug release study was established through the 0.1 N HCl pH 1.2, acetate buffer pH 4.5, and phosphate buffer pH 6.8 with % cumulative drug release of 86.71 ± 8.14 , 85.82 ± 4.58 , and 70.98 ± 5.69 % , was found respectively, compared with the RBO suspension (RBO-SUS). In vitro intestinal gut permeation studies unveiled a 1.95-fold gain in gut permeation by RBO-NLCs compared with RBO-SUS. In vitro lipolysis suggests the drug availability at the absorption site. In vitro haemolysis study suggests the compatibility of NLCs to red blood cells compared to the suspension of the pure drug. The confocal study revealed the depth of penetration of the drug into the intestine by RBO-NLCs which was enhanced compared to RBO-SUS. A cell line study was done in MCF-7 and significantly reduced the IC50 value compared to the pure drug. The in vivo parameters suggested the enhanced bioavailability by 3.54 times of RBO-NLCs as compared to RBO-SUS. Conclusion. The in vitro, ex vivo, and in vivo results showed a prominent potential for bioavailability enhancement of RBO and effective breast cancer therapy.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        pictorial
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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