Aqueous-Core Lipid Nanocapsules for Encapsulating Fragile Hydrophilic and/or Lipophilic Molecules

Abstract

This paper presents the original method of producing aqueous-core lipid nanocapsule, able to encapsulate both hydrophilic and lipophilic species with relevant yields. The scope offered by the integration of both hydrophilic and lipophilic molecules within the same colloidal objects make this method a prime candidate for the numerous anticancer therapies for which chemotherapy frequently requires the association of several molecules. The proof of concept study is proposed here (i) describing in detail the formulation of such objects and their characterization (TEM, cryo-TEM, soft particle analysis), (ii) showing the encapsulation of hydrophilic species alone, using examples of very different molecular weights, such as a dye (methylene blue) and a protein (BSA-isothycianate fluorecein labeled), and (iii) showing the simultaneous encapsulation of hydrophilic (methylene blue) and lipophilic (also a dye, red Sudan III) species.

Interfacial click chemistry for improving both dextran shell density and stability of biocompatible nanocapsules

“…Polymeric nanoparticles 4 (NPs) can be divided into nanospheres (NSs) and nanocapsules (NCs) depending on their 5 structure [4]. Whereas NSs are polymeric matrix systems with a plain and homogeneous 6 structure, NCs are vesicular systems, that exhibit a typical core/shell structure with an inner 7 liquid core surrounded by a polymer coating [4,5]. NCs, thanks to their specific morphology, 8 present many advantages over NSs such as: (i) versatility of encapsulated compounds (either 9 hydrophilic or hydrophobic) depending on their liquid core polarity [6], (ii) high loading 10 capacity related to the liquid core volume and the active substance solubility [4,7], (iii) 11 possibility to modulate the substance release by adjusting nature and thickness of the polymer 12 shell, but also by tuning polarity and volume of the liquid core [8,9], (iv) reduced polymer 13 content [4], (v) protection of encapsulated substance when loaded within the central cavity [4, 14 7].…”

“…Whereas NSs are polymeric matrix systems with a plain and homogeneous 6 structure, NCs are vesicular systems, that exhibit a typical core/shell structure with an inner 7 liquid core surrounded by a polymer coating [4,5]. NCs, thanks to their specific morphology, 8 present many advantages over NSs such as: (i) versatility of encapsulated compounds (either 9 hydrophilic or hydrophobic) depending on their liquid core polarity [6], (ii) high loading 10 capacity related to the liquid core volume and the active substance solubility [4,7], (iii) 11 possibility to modulate the substance release by adjusting nature and thickness of the polymer 12 shell, but also by tuning polarity and volume of the liquid core [8,9], (iv) reduced polymer 13 content [4], (v) protection of encapsulated substance when loaded within the central cavity [4, 14 7]. NCs such as other polymeric nanoparticles (NPs) may also be covered by a hydrophilic 15 shell (for examples polyethylene glycol [10,11] or a neutral, biodegradable and 16 biocompatible polysaccharide such as dextran [12][13][14]) to ensure their colloidal stability or 17 stealthiness in case of drug delivery systems.…”

Phospholipon 90H (P90H)–based PEGylated microscopic lipospheres delivery system for gentamicin: an antibiotic evaluation

“…The amount of drug encapsulated can vary from 1 % to 5 % for hydrophilic compounds and up to 80 % for lipophilic compounds [8,9] . Solid microparticles in dispersions are usually obtained using a melt dispersion method or a solvent evaporation method [10,11] .…”

Organisation structurale et moléculaire des lipides dans les aliments : impacts possibles sur leur digestion et leur assimilation par l’Homme

“…Les nanoparticules structur ees r ealis ees a partir de nano emulsions lipidiques mais utilisant des surfactants et cosurfactants polym eriques sont de plus en plus utilis ees (Anton et al, 2008 ;Huynh et al, 2009 ;Letchford et Burt, 2007). Les nanosph eres sont constitu ees d'une matrice continue dans laquelle le principe actif est uniform ement dispers e alors que les nanocapsules correspondent a des « r eservoirs » o u un coeur aqueux (encapsulation de mol ecules hydrophiles) ou huileux (encapsulation de mol ecules lipophiles) est entour e d'une membrane polym ere (Anton et al, 2008(Anton et al, , 2009Huynh et al, 2009 ;Wawrezinieck et al, 2008). Certaines nanoparticules (NLC pour « nanostructured lipid carrier ») sont produites a partir d'un m elange de lipides solides et liquides (Muchow et al, 2008 ;Muller et Keck, 2004 ;Shidhaye et al, 2008).…”