Formulation of self-nanoemulsifying drug delivery systems containing monoacyl phosphatidylcholine and Kolliphor® RH40 using experimental design

Tran, Thuy Linh; Rades, Thomas

doi:10.1016/j.ajps.2017.09.006

Cited by 29 publications

(14 citation statements)

References 15 publications

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“…Triacetin has also shown a skin penetration enhancement effect [31]. The selected surfactant, Kolliphor ® RH 40 (polyoxyl 40 hydrogenated castor oil), is a non-ionic solubilizer and emulsifying agent [32][33][34]. Its hydrophobic moiety is a combination of glycerol polyethyleneglycol hydroxystearate and fatty acid glycerol polyglycol esters, while the hydrophilic moiety is a combination of polyethylene glycols and glycerol ethoxylate [33].…”

Section: Discussionmentioning

confidence: 99%

Novel Nanocarriers for Targeted Topical Skin Delivery of the Antioxidant Resveratrol

et al. 2020

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Resveratrol (RSV) is a potent lipophilic antioxidant with a low aqueous solubility. Novel nanoformulations have been successfully developed and evaluated to increase the potential of resveratrol as a skin targeting antioxidant. Nanoformulations were prepared using a spontaneous emulsification method, and characterized and evaluated for their capabilities to penetrate/permeate the skin. In nanoformulations, the thermodynamic activity of the RSV penetration into/permeation through the skin was correlated with the thermodynamic activity of the RSV in the formulations. When terpenes were incorporated into the nanoformulations, the permeation of RSV through the skin increased and correlated with an increasing lipophilicity of the terpene. The nanoemulsion containing eugenol showed the highest RSV penetration into the stratum corneum (SC) and the epidermis-dermis-follicle region, whereas the limonene containing nanoemulsion had the highest RSV permeation through the skin (the enhancement ratios, compared to a saturated solution of RSV, were (i) 9.55 and (ii) 12.61, respectively, based on the average RSV amount (i) in each skin region and (ii) permeation through skin).

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Section: Discussionmentioning

confidence: 99%

Novel Nanocarriers for Targeted Topical Skin Delivery of the Antioxidant Resveratrol

et al. 2020

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“…medium-chain mono-diglyceride, and Captex® 300, a medium-chain triglyceride, could enhance permeation via the paracellular pathway by opening the tight junctions while keeping the cytotoxicity at its minimum [35,36]. Besides, in addition to its stabilizing effect as a surfactant, Kolliphor® RH40 is an intestinal permeation enhancer known to increase the membrane permeability [37], and it was reported that it may also act as P-glycoprotein (P-gp) inhibitor [38].…”

Section: Tablementioning

confidence: 99%

Hydrophobic ion pairing of a GLP-1 analogue for incorporating into lipid nanocarriers designed for oral delivery

Ismail

Phan

Laffleur

et al. 2020

European Journal of Pharmaceutics and Biopharmaceutics

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The lipophilic character of peptides can be tremendously improved by hydrophobic ion pairing (HIP) with counterions to be efficiently incorporated into lipid-based nanocarriers (NCs). Herein, HIPs of exenatide with the cationic surfactant tetraheptylammonium bromide (THA) and the anionic surfactant sodium docusate (DOC) were formed to increase its lipophilicity. These HIPs were incorporated into lipid based NCs comprising 41% Capmul MCM, 15% Captex 355, 40% Cremophor RH and 4% propylene glycol. Exenatide-THA NCs showed a log D lipophilic phase (LPh)/release medium (RM) of 2.29 and 1.92, whereas the log D LPh/RM of exenatide-DOC was 1.2 and −0.9 in simulated intestinal fluid and Hanks' balanced salts buffer (HBSS), respectively. No significant hemolytic activity was induced at a concentration of 0.25% (m/v) of both blank and loaded NCs. Exenatide-THA NCs and exenatide-DOC NCs showed a 10-fold and 3-fold enhancement in intestinal apparent membrane permeability compared to free exenatide, respectively. Furthermore, orally administered exenatide-THA and exenatide-DOC NCs in healthy rats resulted in a relative bioavailability of 27.96 ± 5.24% and 16.29 ± 6.63%, respectively, confirming the comparatively higher potential of the cationic surfactant over the anionic surfactant. Findings of this work highlight the potential of the type of counterion used for HIP as key to successful design of lipid-based NCs for oral exenatide delivery.

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“…Another important factor that also affects the oral bioavailability of BCS IV drugs is poor intestinal permeability [3]. Hence, to enhance their solubility, lipid-based formulations have been successfully used as oral delivery systems [4]. Self-nano-emulsifying drug delivery systems (SNEDDS) are one of the most special and interesting lipid-based formulations [4] and are considered as a promising approach for improving the rate and extent of absorption of BCS II or IV drugs [5,6].…”

Section: Introductionmentioning

confidence: 99%

“…Hence, to enhance their solubility, lipid-based formulations have been successfully used as oral delivery systems [4]. Self-nano-emulsifying drug delivery systems (SNEDDS) are one of the most special and interesting lipid-based formulations [4] and are considered as a promising approach for improving the rate and extent of absorption of BCS II or IV drugs [5,6]. SNEDDS are defined as isotropic mixtures of oils, surfactants and co-solvents that have a unique ability of forming a fine oil in water nanoemulsions upon gentle agitation by dilution in an aqueous environment [7][8][9].…”

Section: Introductionmentioning

confidence: 99%

In Vitro Evaluation of Self-Nano-Emulsifying Drug Delivery Systems (SNEDDS) Containing Room Temperature Ionic Liquids (RTILs) for the Oral Delivery of Amphotericin B

et al. 2020

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Amphotericin B (AmpB), one of the most commonly used agents in the treatment of severe fungal infections and life-threatening parasitic diseases such as visceral Leishmaniasis, has a negligible oral bioavailability, primarily due to a low solubility and permeability. To develop an oral formulation, medium chain triglycerides and nonionic surfactants in a self-nano-emulsifying drug delivery system (SNEDDS) containing AmpB were combined with room temperature ionic liquids (RTILs) of imidazolium. The presence of ionic liquids significantly enhanced the solubility of AmpB, exhibited a low toxicity and increased the transport of AmpB across Caco-2 cell monolayers. The combination of RTILs with a lipid formulation might be a promising strategy to improve the oral bioavailability of AmpB.

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Formulation of self-nanoemulsifying drug delivery systems containing monoacyl phosphatidylcholine and Kolliphor® RH40 using experimental design

Cited by 29 publications

References 15 publications

Novel Nanocarriers for Targeted Topical Skin Delivery of the Antioxidant Resveratrol

Novel Nanocarriers for Targeted Topical Skin Delivery of the Antioxidant Resveratrol

Hydrophobic ion pairing of a GLP-1 analogue for incorporating into lipid nanocarriers designed for oral delivery

In Vitro Evaluation of Self-Nano-Emulsifying Drug Delivery Systems (SNEDDS) Containing Room Temperature Ionic Liquids (RTILs) for the Oral Delivery of Amphotericin B

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