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Bromelain-Functionalized Multiple-Wall Lipid-Core Nanocapsules: Formulation, Chemical Structure and Antiproliferative
Catiúscia P Oliveira1,2, Willian A Prado3, Vladimir Lavayen3
1Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil. catipadilha@yahoo.com.br.
Purpose:
This study was conducted a promising approach to surface functionalization developed for lipid-core nanocapsules and the merit to pursue new strategies to treat solid tumors.
Methods:
Bromelain-functionalized multiple-wall lipid-core nanocapsules (Bro-MLNC-Zn) were produced by self-assembling following three steps of interfacial reactions. Physicochemical and structural characteristics, in vitro proteolytic activity (casein substrate) and antiproliferative activity (breast cancer cells, MCF-7) were determined.
Results:
Bro-MLNC-Zn had z-average diameter of 135 nm and zeta potential of +23 mV. The complex is formed by a Zn-N chemical bond and a chelate with hydroxyl and carboxyl groups. Bromelain complexed at the nanocapsule surface maintained its proteolytic activity and showed anti-proliferative effect against human breast cancer cells (MCF-7) (72.6 ± 1.2% at 1.250 μg mL-1 and 65.5 ± 5.5% at 0.625 μg mL-1). Comparing Bro-MLNC-Zn and bromelain solution, the former needed a dose 160-folds lower than the latter for a similar effect. Tripan blue dye assay corroborated the results.
Conclusions:
The surface functionalization approach produced an innovative formulation having a much higher anti-proliferative effect than the bromelain solution, even though both in vitro proteolytic activity were similar, opening up a great opportunity for further studies in nanomedicine.
Insights
This study developed novel bromelain-functionalized lipid-core nanocapsules (Bro-MLNC-Zn) for cancer treatment. These nanocapsules demonstrated significantly enhanced anti-proliferative effects against breast cancer cells compared to free bromelain.
Area of Science:
- Nanomedicine
- Biotechnology
- Cancer Therapy
Background:
- Solid tumors present a significant challenge in cancer treatment.
- Developing novel drug delivery systems is crucial for improving therapeutic efficacy.
- Surface functionalization of nanocarriers offers a promising strategy for targeted therapy.
Purpose of the Study:
- To develop and characterize bromelain-functionalized multiple-wall lipid-core nanocapsules (Bro-MLNC-Zn).
- To evaluate the in vitro proteolytic and anti-proliferative activities of Bro-MLNC-Zn.
- To compare the efficacy of Bro-MLNC-Zn with free bromelain for breast cancer treatment.
Main Methods:
- Bro-MLNC-Zn were synthesized using a self-assembly process with interfacial reactions.
- Physicochemical properties (size, zeta potential) and structural characteristics were analyzed.
- In vitro assays were performed to determine proteolytic activity (casein substrate) and anti-proliferative effects on MCF-7 breast cancer cells.
Main Results:
- Bro-MLNC-Zn exhibited a z-average diameter of 135 nm and a zeta potential of +23 mV.
- The nanocapsules maintained bromelain's proteolytic activity and showed significant anti-proliferative effects on MCF-7 cells.
- Bro-MLNC-Zn required a 160-fold lower dose than free bromelain to achieve similar anti-proliferative effects.
Conclusions:
- Surface functionalization of lipid-core nanocapsules with bromelain creates an innovative formulation.
- Bro-MLNC-Zn demonstrates superior anti-proliferative efficacy compared to free bromelain, despite similar proteolytic activity.
- This approach holds significant potential for nanomedicine applications in treating solid tumors.
