An insight of in vitro transport of PEGylated non-ionic surfactant vesicles (NSVs) across the intestinal polarized enterocyte monolayers

Non-ionic surfactant vesicles was developed and characterized for ophthalmic drug delivery of Diclofenac potassium. The present research study is a promising approach to improve corneal penetration and bioavailability characteristics. Formulation also found to ensure a good entrapment efficiency and ocular bioavailability of drug in-vivo. Non-ionic surfactant vesicles containing Diclofenac potassium were prepared using surfactant and cholesterol in different ratio by Lipid film hydration technique. Niosomes were characterized For Entrapment efficiency, Particle size analysis, In-vitro drug release and In-vivo studies. The best formulation selected based on above parameters were subjected for sustained release study. Formulation with low cholesterol content which shown 82.1% Entrapment efficiency, 70.01% sustained release over a period of 10 h followed a non-fickian profile with zero order release profile. Scanning electron micrograph indicated that Niosomes have a discrete spherical structure without aggregation. In-vivo study showed an availability of drug in aqueous humor for an extended time period even up to 8 hour and it showed a correlation with the release profile in-vitro. Non-ionic surfactant vesicles are considered the best as it showed good and high Entrapment efficiency and Vitro release with better bioavailability. The proposed method was found to be precise and selective for the development and characterization of Diclofenac potassium Niosomes. Key words: Diclofenac potassium, corneal penetration, sorbitan mono stearate, Entrapment efficiency, SEM, in vitro release study, HPLC.

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In-Vitro Application of Magnetic Hybrid Niosomes: Targeted siRNA-Delivery for Enhanced Breast Cancer Therapy

Pharmaceutics ◽

10.3390/pharmaceutics13030394 ◽

2021 ◽

Vol 13 (3) ◽

pp. 394 ◽

Cited By ~ 1

Author(s):

Viktor Maurer ◽

Selin Altin ◽

Didem Ag Seleci ◽

Ajmal Zarinwall ◽

Bilal Temel ◽

...

Keyword(s):

Breast Cancer ◽

Cellular Uptake ◽

Sirna Delivery ◽

Superparamagnetic Iron Oxide ◽

Cost Effective ◽

Chemotherapeutic Agents ◽

Therapy Outcome ◽

Ionic Surfactant ◽

Combinational Therapy

Even though the administration of chemotherapeutic agents such as erlotinib is clinically established for the treatment of breast cancer, its efficiency and the therapy outcome can be greatly improved using RNA interference (RNAi) mechanisms for a combinational therapy. However, the cellular uptake of bare small interfering RNA (siRNA) is insufficient and its fast degradation in the bloodstream leads to a lacking delivery and no suitable accumulation of siRNA inside the target tissues. To address these problems, non-ionic surfactant vesicles (niosomes) were used as a nanocarrier platform to encapsulate Lifeguard (LFG)-specific siRNA inside the hydrophilic core. A preceding entrapment of superparamagnetic iron-oxide nanoparticles (FexOy-NPs) inside the niosomal bilayer structure was achieved in order to enhance the cellular uptake via an external magnetic manipulation. After verifying a highly effective entrapment of the siRNA, the resulting hybrid niosomes were administered to BT-474 cells in a combinational therapy with either erlotinib or trastuzumab and monitored regarding the induced apoptosis. The obtained results demonstrated that the nanocarrier successfully caused a downregulation of the LFG gene in BT-474 cells, which led to an increased efficacy of the chemotherapeutics compared to plainly added siRNA. Especially the application of an external magnetic field enhanced the internalization of siRNA, therefore increasing the activation of apoptotic signaling pathways. Considering the improved therapy outcome as well as the high encapsulation efficiency, the formulated hybrid niosomes meet the requirements for a cost-effective commercialization and can be considered as a promising candidate for future siRNA delivery agents.

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