Lipomatrix: A Novel Ascorbyl Palmitate-Based Lipid Matrix to Enhancing Enteric Absorption of Serenoa Repens Oil.

Andrea Fratter,Stefano Valier,Marzia Pellizzato,Arrigo Cicero,Erik Tedesco,Vera Mason,Federico Benetti,Elisa Meneghetti

doi:10.3390/ijms20030669

Andrea Fratter, Stefano Valier + Show 6 more

Open Access

https://doi.org/10.3390/ijms20030669

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Abstract

The class of lipophilic compounds coming from vegetal source represents a perspective in the adjuvant treatment of several human diseases, despite their poor bioavailability in humans. These compounds are generally soluble in fats and poorly soluble in water. The major reason for the poor bioavailability of lipophilic natural compounds after oral uptake in humans is related to their reduced solubility in enteric water-based fluids, leading to an ineffective contact with absorbing epithelium. The main goal to ensure efficacy of such compounds is then creating technological conditions to deliver them into the first enteric tract as hydro-dispersible forms to maximize epithelial absorption. The present work describes and characterizes a new technological matrix (Lipomatrix, Labomar Research, Istrana, TV, Italy) based on a molten fats core in which Ascorbyl Palmitate is embedded, able to deliver lipophilic compounds in a well-dispersed and emulsified form once exposed to duodenal fluids. Authors describe and quantify Lipomatrix delivery of Serenoa repens oil through an innovative in vitro model of human gastro-enteric digestion, reporting results of its improved bioaccessibility, enteric absorption and efficacy compared with not formulated Serenoa repens oil-containing commercial products using in vitro models of human intestine and prostatic tissue.

Highlights

Natural compounds with specific reference to plant-derived active ingredients are raising interest as coadjuvant treatment of human diseases
Differential Scanning Calorimetry (DSC) analysis was performed on mono and diglycerides of fatty acids (MDGFA), mannitol, ascorbyl palmitate (ASP), SRO, and Lipomatrix as described in Section 3.2.1.2, in order to evaluate possible changes in the crystallinity structure of the single raw material once embedded into the matrix and thereby speculate on its prevalent amorphous or crystalline state
From the analysis of the Lipomatrix thermogram achieved in the range temperature of 25–125 ◦C (Supplementary file) it is possible to recognize a melting pick between 47 and 55 ◦C coherent with the melting point of MDGFA even though there is a significant decrease in the melting temperature pick of about 10 ◦C in respect to MDGFA alone

Summary

Introduction

Natural compounds with specific reference to plant-derived active ingredients are raising interest as coadjuvant treatment of human diseases. In recent years, this trend has consolidated and many natural products have been introduced into the market under the label of nutritional supplements (NS) or foods with special medical purposes (SMPF). Despite the effective and charming marketing efforts of companies in selling these products following medical routes, the real efficacy of nutraceuticals is. 2019, 20, x FOR PEER REVIEW still a challenging issue because of the inadequate technological framework for enhancing and testing theoifr nbuiotraavcaeiulatibciallistyi.s still a challenging issue because of the inadequate technological framework for enhLaipnocipnhgilaincdactetisvtienigntghreeidr ibeinotasvbaeillaobnilgitiyn.g to the families of terpens, saponins, and vegetal oils are poorly Laibpsooprhbielidc bacytiivneteinsgtirneedimenatisnblyelobnegcainugsetootfhtehfeaimr illoiews owf ateterpr esnosl,usbaipliotnyin[1s,,2a]n. Sci. 2019, 20, x FOR PEER REVIEW still a challenging issue because of the inadequate technological framework for enhancing and testing theoifr nbuiotraavcaeiulatibciallistyi.s still a challenging issue because of the inadequate technological framework for enhLaipnocipnhgilaincdactetisvtienigntghreeidr ibeinotasvbaeillaobnilgitiyn.g to the families of terpens, saponins, and vegetal oils are poorly Laibpsooprhbielidc bacytiivneteinsgtirneedimenatisnblyelobnegcainugsetootfhtehfeaimr illoiews owf ateterpr esnosl,usbaipliotnyin[1s,,2a]n. dTvheegientatelroaiclstiaorne of actpivoeorcloymapbsoournbdeds wbyithinitnestetisnteinmalaeipnliythbeelicuamusde eopfetnhdeisrolnowthwe datiesrsosloultuiboinlitoyf m[1,o2l]e. cTuhleesinintewraactteior-nbaosfed intaecsttiivneacloflmupiodusn[d3s].wiAth ivnitsecsotiunsalmepuicthoeploiulymsadcecpheanrdids eosn trhicehdilsasyoelurtisotnricotflmy oaldechuelreisnign wtoattehre-beansetderic peplaiie1ytnp)hstiepetalshliatupeiynlmiisvauolamatnfapladluinvrisdodoylstesnaylt[inh3nr]teo.hrsleeeiAgzsieiunzdvleairdbsteicygnbougysulpsastehpticmeenicagauilbacitzlsohieozpedreopadlGbtyiGsosooaobncrblpcerlhatetiattcoerecnielodllrsfelas,sa,tccecartailiovlcleflheedadiclnuatuginynvrseesetrtidirirnisrretegerndridtceswtdw.lyiaMaettneaeutrdrsc.hpipneMhhsraa,iunssiceengidn((UUtseo,eWWdintP,Phdc)e)e,,ae(n(eFFdniii,gntgecuturaerirnreceac1t) witinhtperoaocrtlwy-istholpuobolerlmy-osolelucublleesmporleevcuenletsinpgretvheenirtipnegntehteriartpioenne[t4r,a5t]i.on [4,5]

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