Molecular insights into the formation of drug-monoacyl phosphatidylcholine solid dispersions for oral delivery

Gautschi, Nicolas; Hoogevest, Peter van; Kuentz, Martin

doi:10.1016/j.ejps.2016.05.023

Cited by 10 publications

(3 citation statements)

References 43 publications

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“…the degree of amorphization, storage stability or processability) should also be considered. Due to different (molecular) interactions between drug compound and phospholipid the applicability of mono-vs diacyl phospholipid as excipients in solid dispersions may vary between different drug compounds as shown for monoacyl PC (Gautschi et al, 2017).…”

Section: Accepted Manuscriptmentioning

confidence: 99%

A dynamic in vitro permeation study on solid mono- and diacyl-phospholipid dispersions of celecoxib

Jacobsen

Elvang

Bauer‐Brandl

et al. 2019

European Journal of Pharmaceutical Sciences

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Section: Accepted Manuscriptmentioning

confidence: 99%

A dynamic in vitro permeation study on solid mono- and diacyl-phospholipid dispersions of celecoxib

Jacobsen

Elvang

Bauer‐Brandl

et al. 2019

European Journal of Pharmaceutical Sciences

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“…As such, it is hypothesized that they form an excellent basis for both poorly water-soluble lipophilic compounds ("grease ball" molecules) and poorly water-soluble compounds with high melting points ("brick dust" molecules), and thus may be broadly applicable. In this context, the project of Thomas Rades (University of Copenhagen, Copenhagen, Denmark) is envisaged to investigate the potential use of lecithin [10] as a co-former to develop co-amorphous solid dispersions for a range of poorly water-soluble drugs [172][173][174][175][176]. Additionally, the use of co-amorphous drug lecithin systems as a new source of drug-forms to be added to lipid-based drug delivery systems (self nano-emulsifying drug delivery systems (SNEDDS)) will be investigated.…”

Section: Principalmentioning

confidence: 99%

The Phospholipid Research Center: Current Research in Phospholipids and Their Use in Drug Delivery

Drescher

Hoogevest

2020

Pharmaceutics

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This review summarizes the research on phospholipids and their use for drug delivery related to the Phospholipid Research Center Heidelberg (PRC). The focus is on projects that have been approved by the PRC since 2017 and are currently still ongoing or have recently been completed. The different projects cover all facets of phospholipid research, from basic to applied research, including the use of phospholipids in different administration forms such as liposomes, mixed micelles, emulsions, and extrudates, up to industrial application-oriented research. These projects also include all routes of administration, namely parenteral, oral, and topical. With this review we would like to highlight possible future research directions, including a short introduction into the world of phospholipids.

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“…Phosphatidylcholine (PC) is amphiphilic in nature and is composed of an esterified glycerol backbone with fatty acids and a choline head. 15 , 16 Its biocompatible and amphiphilic characteristics have been applied as a solubilizer in diverse pharmaceutical formulations. 16 The hydrophilic choline head group is zwitterionic and consists of a positively charged quaternary amine and a negatively charged phosphate group.…”

Section: Introductionmentioning

confidence: 99%

Combined Orobol-Bentonite Composite Formulation for Effective Topical Skin Targeted Therapy in Mouse Model

Nguyen¹,

Kim²,

Yu³

et al. 2022

IJN

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Orobol is an isoflavone that has a potent skin protection effect. The objective of this study was to prepare a novel bentonitebased composite formulation of orobol to enhance topical skin delivery. Methods: The composition was optimized based on the orobol content in the composite and the in vitro release studies, followed by the in vitro and in vivo hairless mouse skin deposition studies. Physicochemical characterizations of the composite formulation were performed by powder X-ray refractometry (XRD) and scanning electron microscopy (SEM). The in vitro cytotoxicity and in vivo toxicity studies were conducted in human keratinocytes and in hairless mouse, respectively. Results and Discussions:The in vitro release of orobol from the bentonite composites was higher than that from the suspension, which was further increased with the addition of phosphatidylcholine. The composite formulation significantly enhanced the in vitro and in vivo skin deposition of orobol in hairless mouse skin compared to the orobol suspension. Moreover, the addition of phosphatidyl choline not only improved the dissolution and incomplete release of orobol from the bentonite composite but also enhanced the deposition of orobol in the skin. XRD histograms and SEM images confirmed that the enhanced dissolution of orobol from the composite was attributed to its amorphous state on bentonite. The in vitro and in vivo toxicity studies support the safety and biocompatibility of the orobol-loaded bentonite composite formulation. Conclusion: These findings suggest that the orobol-loaded bentonite composite formulation could be a potential topical skin delivery system for orobol.

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Molecular insights into the formation of drug-monoacyl phosphatidylcholine solid dispersions for oral delivery

Cited by 10 publications

References 43 publications

A dynamic in vitro permeation study on solid mono- and diacyl-phospholipid dispersions of celecoxib

A dynamic in vitro permeation study on solid mono- and diacyl-phospholipid dispersions of celecoxib

The Phospholipid Research Center: Current Research in Phospholipids and Their Use in Drug Delivery

Combined Orobol-Bentonite Composite Formulation for Effective Topical Skin Targeted Therapy in Mouse Model

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