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Open AccessArticle

Copolymeric Micelles Overcome the Oral Delivery Challenges of Amphotericin B

1
Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, Thailand
2
Clinical and Health Sciences, University of South Australia, Adelaide, SA 5000, Australia
3
The Center of Excellence for Innovation in Chemistry (PERCH-CIC), Department of Chemistry, Faculty of Science, Mahidol University, Bangkok 10400, Thailand
4
ARC Centre of Excellence in Convergent Bio-Nano Science & Technology, University of South Australia, Adelaide, SA 5000, Australia
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(6), 121; https://doi.org/10.3390/ph13060121
Received: 19 May 2020 / Revised: 7 June 2020 / Accepted: 9 June 2020 / Published: 11 June 2020
(This article belongs to the Section Pharmaceutical Technology)
Classified as a Biopharmaceutical Classification System (BCS) class IV drug, amphotericin B (AmB) has low aqueous solubility and low permeability leading to low oral bioavailability. To improve these limitations, this study investigated the potential of AmB-loaded polymeric micelles (AmB-PM) to increase intestinal absorption. AmB-PM were prepared with polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol copolymer (Soluplus®) as a polymeric carrier and used a modified solvent diffusion and microfluidics (NanoAssemblr®) method. AmB-PM have a mean particle size of ~80 nm and are mono-disperse with a polydispersity index <0.2. The entrapment efficiency of AmB was up to 95% and achieved with a high drug loading up to ~20% (w/w) with a total amount of incorporated drug of 1.08 ± 0.01 mg/mL. Importantly, compared to free drug, AmB-PM protected AmB from degradation in an acidic (simulated gastric) environment. Viability studies in Caco-2 cells confirmed the safety/low toxicity of AmB-PM. In vitro cellular absorption studies confirmed that AmB-PM increased AmB uptake in Caco-2 cells 6-fold more than free AmB (i.e., 25% compared with 4% within 30 min). Furthermore, the permeability of AmB across Caco-2 monolayers was significantly faster (2-fold) and more pronounced for AmB-PM in comparison to free drug (3.5-fold increase). Thus, the developed AmB-PM show promise as a novel oral delivery system for AmB and justifies further investigation. View Full-Text
Keywords: amphotericin B; Soluplus®; polymeric micelles; oral absorption; caco-2 cells; cellular uptake amphotericin B; Soluplus®; polymeric micelles; oral absorption; caco-2 cells; cellular uptake
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Nimtrakul, P.; Williams, D.B.; Tiyaboonchai, W.; Prestidge, C.A. Copolymeric Micelles Overcome the Oral Delivery Challenges of Amphotericin B. Pharmaceuticals 2020, 13, 121.

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