Production and characterization of testosterone undecanoate-loaded NLC for oral bioavailability enhancement

Muchow, Marc; Maincent, Philippe; Müller, Rainer H.; Keck, Cornelia M.

doi:10.3109/03639045.2010.489559

Cited by 34 publications

(17 citation statements)

References 19 publications

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“…For instance, Muchow et al . observed that small sized NLCs (200 nm) showed higher AUC values in comparison to higher sized NLCs (600 nm) when administered orally to rats, this was attributed to their higher mucoadhesion capability in the body [36]. …”

Section: Fabrication Of Nlcsmentioning

confidence: 99%

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Poonia¹,

Kharb

Lather³

et al. 2016

Future Sci. OA

146

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Oral delivery is the most accepted and economical route for drug administration and leads to substantial reduction in dosing frequency. However, this route still remains a challenge for the pharmaceutical industry due to poorly soluble and permeable drugs leading to poor oral bioavailability. Incorporating bioactives into nanostructured lipid carriers (NLCs) has helped in boosting their therapeutic functionality and prolonged release from these carrier systems thus providing improved pharmacokinetic parameters. The present review provides an overview of noteworthy studies reporting impending benefits of NLCs in oral delivery and highlights recent advancements for developing engineered NLCs either by conjugating polymers over their surface or modifying their charge to overcome the mucosal barrier of GI tract for active transport across intestinal membrane.

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Section: Fabrication Of Nlcsmentioning

confidence: 99%

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Poonia¹,

Kharb

Lather³

et al. 2016

Future Sci. OA

146

View full text Add to dashboard Cite

show abstract

“…21 Recently, NLCs have been investigated to improve the oral bioavailability of poorly water-soluble drugs. [22][23][24][25][26] In this study, SM-loaded NLCs (SM-NLCs) were prepared by a high-pressure homogenization method and characterized for particle size, entrapment efficiency, morphology, in vitro lipolysis, and in vitro release. The preparative variables were optimized.…”

Section: Introductionmentioning

confidence: 99%

Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin

Shangguan

Lü

et al. 2013

J Biomater Appl

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The main purpose of this study was to prepare binary lipids-based nanostructured lipid carriers to improve the oral bioavailability of silymarin, a poorly water-soluble liver protectant. Silymarin-loaded nanostructured lipid carriers were prepared by the method of high-pressure homogenization with glycerol distearates (Precirol ATO-5) and oleic acid as the solid and liquid lipids, respectively, and lecithin (Lipoid E 100) and Tween-80 as the emulsifiers. The silymarin-nanostructured lipid carrier prepared under optimum conditions was spherical in shape with mean particle size of ∼78.87 nm, entrapment efficiency of 87.55%, loading capacity of 8.32%, and zeta potential of -65.3 mV, respectively. In vitro release of silymarin-nanostructured lipid carriers was very limited even after 12 h, while in vitro lipolysis showed fast digestion of nanostructured lipid carriers within 1 h. Relative oral bioavailability of silymarin-nanostructured lipid carriers in Beagle dogs was 2.54- and 3.10-fold that of marketed Legalon® and silymarin solid dispersion pellets, respectively. It was concluded that nanostructured lipid carriers were potential drug delivery systems to improve the bioavailability of silymarin. Other than improved dissolution, alternative mechanisms such as facilitated absorption as well as lymphatic transport may contribute to bioavailability enhancement.

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“…The terminal alkene of uC 11 reduces its hydrophobicity compared to the saturated C 11 salt, with a resultant increase in solubility and critical micelle concentration (CMC) (15,16). UA and its salts have been used as penetration enhancers in transdermal drug delivery (17,18), and there have been attempts to improve oral delivery of testosterone using a UA ester (19,20); however, the use of either UA and/or uC 11 specifically as intestinal permeation enhancers has never been investigated. uC 11 is a powder, more amenable to commercial-scale solid dose manufacturing than the acid form and was therefore more appropriate for the current oral drug delivery study.…”

Section: Introductionmentioning

confidence: 99%

Efficacious Intestinal Permeation Enhancement Induced by the Sodium Salt of 10-undecylenic Acid, A Medium Chain Fatty Acid Derivative

Brayden

Walsh

2014

AAPS J

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ABSTRACT. 10-undecylenic acid (UA) is an OTC antifungal therapy and a nutritional supplement. It is an unsaturated medium chain fatty acid (MCFA) derivative, so our hypothesis was that its 11-mer sodium salt, uC 11 , would improve intestinal permeation similar to the established enhancer, sodium caprate (C 10 ), but without the toxicity of the parent saturated MCFA, decylenic acid (C 11 ). MTT assay and high-content screening (HCS) confirmed a cytotoxicity ranking in Caco-2 cells: C 11 >C 10 =uC 11 . Five to ten millimolars of the three agents reduced TEER and increased the Papp of [ 14 C]-mannitol across Caco-2 monolayers and rat intestinal mucosae, a concentration that matched increases in plasma membrane permeability seen in HCS. Although C 11 was the most efficacious enhancer in vitro, it damaged monolayers and tissue mucosae more than the other two agents at similar concentrations and exposure times and was therefore not pursued further. Rat jejunal and colonic in situ intestinal instillations of 100 mM C 10 or uC 11 with FITC-dextran 4000 (FD4) solutions yielded comparable regional enhancement ratios of~10 and 30%, respectively, for each agent with acceptable tissue histology. Mini-tablets of uC 11 and FD4 however delivered more FD4 compared to C 10 -FD-4 mini-tablets in both regions, as reflected by a statistically higher AUC, and with no evidence of membrane perturbation. The unsaturated bond in uC 11 therefore confers a reduction in lipophilicity and cytotoxicity compared to C 11 , and the resulting permeation enhancement is on a par with or superior to that of C 10 , a key component of formulations in current phase II oral peptide clinical trials.

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Production and characterization of testosterone undecanoate-loaded NLC for oral bioavailability enhancement

Abstract: This opens the perspective of administering a single dose of dose of TU in one oral dosage unit and simultaneously having a bioavailability less dependent on the fed state.

Cited by 34 publications

References 19 publications

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin

Efficacious Intestinal Permeation Enhancement Induced by the Sodium Salt of 10-undecylenic Acid, A Medium Chain Fatty Acid Derivative

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