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Ribociclib Nanostructured Lipid Carrier Aimed for Breast Cancer: Formulation Optimization, Attenuating In Vitro
Ali Sartaj1, Annu1, Largee Biswas2
1Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India.
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.
Insights
This study developed oral nanostructured lipidic carriers (NLCs) for Ribociclib (RBO) to improve breast cancer treatment. The RBO-NLCs significantly enhanced drug bioavailability and efficacy compared to the standard suspension.
Area of Science:
- Pharmaceutical Nanotechnology
- Drug Delivery Systems
- Oncology Therapeutics
Background:
- Breast cancer treatment often faces challenges with chemotherapeutic drug bioavailability.
- Ribociclib (RBO) is a key drug for breast cancer, but its oral administration is limited by poor bioavailability.
- Nanostructured lipidic carriers (NLCs) offer a promising approach to enhance oral drug delivery.
Purpose of the Study:
- To develop and evaluate oral nanostructured lipidic carriers (NLCs) for Ribociclib (RBO).
- To overcome the bioavailability limitations of RBO for effective breast cancer therapy.
- To optimize RBO-NLC formulation using a Box-Behnken design (BBD).
Main Methods:
- RBO-NLCs were prepared using the solvent evaporation method and optimized via BBD.
- Characterization included particle size, polydispersity index, entrapment efficiency, and TEM structural analysis.
- In vitro, ex vivo, and in vivo studies were conducted to assess drug release, permeation, lipolysis, haemolysis, intestinal penetration, and bioavailability.
Main Results:
- Optimized RBO-NLCs showed a particle size of 114.23 nm, PDI of 0.649, and high entrapment efficiency (87.7%).
- In vitro studies demonstrated sustained drug release and significantly enhanced intestinal permeation (1.95-fold).
- In vivo studies confirmed a 3.54-fold increase in RBO bioavailability and reduced IC50 in MCF-7 cells.
Conclusions:
- The developed RBO-NLCs show significant potential for enhancing oral bioavailability.
- These NLCs offer a promising strategy for improved breast cancer therapy.
- The study highlights the efficacy of NLCs for overcoming drug delivery challenges in cancer treatment.
