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Updated: Sep 1, 2025
Monitoring of Nanodrug Accumulation in Murine Breast Cancer Metastases
Published on: August 23, 2024
Oral sorafenib-loaded microemulsion for breast cancer: evidences from the in-vitro evaluations and pharmacokinetic
Nishtha Chaurawal1, Charu Misra1, Harshita Abul Barkat2
1Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan, 305817, India.
Abstract:
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.
Insights
This study developed a novel phospholipid microemulsion for sorafenib tosylate (SFB), enhancing its oral bioavailability and efficacy for breast cancer treatment while reducing toxicity. The nanoformulation shows promise for safer and more effective oral chemotherapy.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Oncology
Background:
- Sorafenib tosylate (SFB) is a multikinase inhibitor used for breast cancer but faces challenges with toxicity, drug resistance, and poor oral bioavailability due to its Biopharmaceutical Classification System (BCS) II status.
- Developing effective drug delivery systems is crucial to overcome these limitations and improve therapeutic outcomes.
Purpose of the Study:
- To encapsulate SFB into a biocompatible and biodegradable phospholipid-based microemulsion (ME) to enhance its oral bioavailability and therapeutic efficacy.
- To characterize the SFB-loaded ME and evaluate its performance in vitro and in vivo.
Main Methods:
- Preparation and characterization of SFB-loaded microemulsion (SFB-loaded ME), including surface charge, morphology, micromeritics, and drug release studies.
- In vitro cell viability assays on 4T1 cell lines to determine IC50 values.
- Pharmacokinetic studies to assess oral bioavailability compared to free SFB.
Main Results:
- The SFB-loaded ME demonstrated controlled drug release and reduced protein binding, increasing drug availability for pharmacological action.
- Cell viability assays showed an enhanced IC50 value for SFB-loaded ME compared to naïve SFB on 4T1 cell lines.
- Pharmacokinetic studies confirmed significantly enhanced oral bioavailability of SFB when formulated as a nanocarrier.
Conclusions:
- The developed phospholipid-based SFB-loaded ME is a promising nanocarrier for oral administration, improving drug bioavailability and potentially offering a safer and more effective cancer chemotherapy option.
- This nanoformulation presents a viable strategy for overcoming the limitations of conventional sorafenib tosylate therapy.
