Comparison of improvements of aqueous dissolution of structurally analogous hydrophobic drugs by amorphous solid dispersion

Okamoto, Takashi; Yamamoto, Kayoko; Sekitoh, Takanari; Fujioka, Akiho; Imanaka, Hiroyuki; Ishida, Naoyuki; Imamura, Koreyoshi

doi:10.1016/j.colsurfa.2021.127744

Cited by 6 publications

(2 citation statements)

References 42 publications

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“…6,7 The dispersion of solid carriers could increase the dissolution surface area of drugs by improving the dissolution rate of waterinsoluble drugs as well as their bioavailability, and this has good prospects for commercial development. 8,9 The widely used ASD carriers can be divided into polymer carriers and inorganic nanocarriers according to their physical properties and stability mechanisms. 10,11 Various methods have been used to prepare solid dispersion systems, such as the melt extrusion method, super critical fluid technology, and electrospinning.…”

Section: Introductionmentioning

confidence: 99%

“…Amorphous drugs have higher apparent solubility than crystalline drugs 6,7 . The dispersion of solid carriers could increase the dissolution surface area of drugs by improving the dissolution rate of water‐insoluble drugs as well as their bioavailability, and this has good prospects for commercial development 8,9 . The widely used ASD carriers can be divided into polymer carriers and inorganic nanocarriers according to their physical properties and stability mechanisms 10,11 …”

Section: Introductionmentioning

confidence: 99%

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Preparation of astaxanthin‐loaded composite micelles with coaxial electrospray technology for enhanced oral bioavailability and improved antioxidation capability

Liao,

Wang,

et al. 2023

J Sci Food Agric

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BackgroundAstaxanthin is approved by Food and Drug Administration (FDA) as a safe dietary supplement for humans. Astaxanthin, as a potent lipid‐soluble keto‐carotenoid, is widely used in food, cosmetics and pharmaceutical fields. However, the low solubility of astaxanthin limits its powerful biological activity and application in the aforementioned fields. This study aims to develop a delivery system to address the low solubility and bioavailability of astaxanthin and to enhance its antioxidant capacity.ResultsAstaxanthin‐loaded Composite Micelles were successfully prepared via Coaxial Electrospray Technology. Astaxanthin was existed in the amorphous state in the electro‐sprayed formulation with an approximate particle size of 186.28 nm with a polydispersity index of 0.243. In this delivery system, Soluplus and copovidone (PVPVA 64) were the main polymeric matrix for astaxanthin, which then released the drug upon contact with aqueous media, and results in an overall increase of drug solubility and a release rate of 94.08 %. Meanwhile, lecithin and PEG‐g‐CS could support the absorption of astaxanthin in the gastrointestinal tract and help the transmembrane transport. Consequently, the relative bioavailability reached about 308.33% and the ROS scavenging efficiency of formulation was 44.10 %, which was 1.57 times higher than that of free astaxanthin (28.10 %) when both were at the same concentration level based on astaxanthin.ConclusionIt could be deduced that coaxial electrospray could be applied to prepare a composite micelles system for the delivery of poorly water‐soluble active ingredients found in the fields of functional food, cosmetics and medicine.This article is protected by copyright. All rights reserved.

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