Related Experiment Video
Updated: Jan 7, 2026
Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
Formulation and Evaluation of Alginate Microcapsules Containing an Uncompetitive Nanomolar Dimeric Indenoindole
Krisztina Bodnár1,2, Christelle Marminon3, Florent Perret4
1Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, 4002 Debrecen, Hungary.
Abstract:
Background/Objectives: The ABCG2 transporter actively effluxes anticancer drugs, reducing their efficacy and promoting multidrug resistance (MDR). Developing oral formulations of poorly soluble ABCG2 inhibitors remains challenging due to their low solubility and intestinal permeability. This study aimed to formulate and evaluate an ABCG2 inhibitor using micro- and nanoscale drug delivery systems. Methods: To address the poor solubility and bioavailability of the corresponding active ingredient, a self-nanoemulsifying drug delivery system (SNEDDS) was developed. The SNEDDS was encapsulated into microcapsules using sodium alginate crosslinked with calcium chloride. Five microcapsule formulations were developed, varying in the inclusion of polyvinylpyrrolidone (PVP), Transcutol® HP and SNEDDS. The effects of the excipients on encapsulation efficiency, swelling capacity, enzymatic stability, dissolution, cytocompatibility, and permeability were systematically evaluated. Results: The SNEDDS exhibited monodisperse particle sizes and efficient drug entrapment. Results revealed that formulations incorporating PVP and SNEDDS improved encapsulation efficiency and bioavailability. SNEDDS-containing formulations demonstrated superior enzymatic stability in simulated gastric and intestinal fluids and provided the highest cumulative drug release in vitro. Cytotoxicity studies conducted on Caco-2 and MCF-7 cells demonstrated that our formulations were well tolerated, indicating favorable biocompatibility. Conclusions: Our findings demonstrate that SNEDDS-loaded alginate microcapsules offer an efficient platform for oral delivery of dimeric ABCG2 inhibitors, combining enhanced solubility, stability, and controlled release. The optimized formulation can be regarded as a promising strategy to enhance the oral bioavailability of efflux pump inhibitors and other poorly soluble drugs.
Insights
This study developed novel alginate microcapsules loaded with self-nanoemulsifying drug delivery systems (SNEDDS) to improve oral delivery of ABCG2 inhibitors, enhancing drug solubility and bioavailability for cancer therapy.
Area of Science:
- Pharmacology
- Materials Science
- Nanotechnology
Background:
- The ABCG2 transporter contributes to multidrug resistance (MDR) by effluxing anticancer drugs, reducing treatment efficacy.
- Poor solubility and low intestinal permeability of ABCG2 inhibitors hinder the development of effective oral formulations.
- Developing advanced drug delivery systems is crucial to overcome these challenges in cancer therapy.
Purpose of the Study:
- To formulate and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) encapsulated in alginate microcapsules for oral delivery of ABCG2 inhibitors.
- To investigate the impact of excipients like polyvinylpyrrolidone (PVP) and Transcutol® HP on formulation performance.
- To assess the solubility, stability, dissolution, cytocompatibility, and permeability of the developed microcapsule formulations.
Main Methods:
- Development of SNEDDS to address poor solubility of the active pharmaceutical ingredient.
- Encapsulation of SNEDDS into sodium alginate microcapsules crosslinked with calcium chloride.
- Systematic evaluation of formulation parameters including encapsulation efficiency, swelling, enzymatic stability, dissolution, and cell-based assays (Caco-2, MCF-7).
Main Results:
- SNEDDS exhibited monodisperse particle size and efficient drug entrapment.
- Formulations with PVP and SNEDDS showed improved encapsulation efficiency and bioavailability.
- SNEDDS-loaded microcapsules demonstrated enhanced enzymatic stability and superior in vitro drug release.
- Cytotoxicity studies confirmed favorable biocompatibility of the developed formulations.
Conclusions:
- SNEDDS-loaded alginate microcapsules provide an effective platform for the oral delivery of dimeric ABCG2 inhibitors.
- The optimized formulation enhances drug solubility, stability, and controlled release, leading to improved oral bioavailability.
- This strategy holds promise for enhancing the efficacy of efflux pump inhibitors and other poorly soluble drugs in cancer treatment.
