Solidification of Nanostructured Lipid Carriers Loaded Testosterone Undecanoate: In Vivo and In Vitro Study

Hua, Yabing; Li, Wanqing; Zhang, Cheng; Zhao, Ziming; Yin, Xiaoxing; Liu, Ying; Sun, Jin; Gao, Jing; Zhang, Hui; Zheng, Aiping

doi:10.1055/a-0573-9132

Cited by 3 publications

(1 citation statement)

References 37 publications

(38 reference statements)

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“…Nonionic surfactants such as sorbitan esters (so called Tweens or Spans) are frequently used in drug delivery systems due to their low toxicity, lack of irritability, and capability to easily form different types of nanocarriers [16]. Span 80 is a lipophilic liquid emulsifying agent which tends to form water-in-oil (W/O) emulsions [17].…”

Section: Introductionmentioning

confidence: 99%

Optimization of Olive Oil-Based Nanoemulsion Preparation for Intravenous Drug Delivery

2018

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A seven-factor Box-Behnken design was used for the optimized development of an olive oil-based nanoemulsion (NE) intended for intravenous drug delivery. The independent variables of olive oil concentration, tween 80 concentration, span 80 concentration, rate of adding of oil in aqueous phase, homogenization speed, homogenization time, and preparation temperature, were used as inputs of the factorial design. The response variables were mean droplet diameter, zeta potential (ZP), and polydispersity index (PDI). A quadratic, linear and 2FI model was established to predict the responses based on the multivariate model developed. The obtained experimental responses were in good agreement with predicted values from expert design, showing residual standard error (RSE) less than 10 %. TEM revealed that the optimized nanoemulsions were almost spherical with mean diameter about 40 nm. The developed formulation showed only about 4.6% of hemolysis and was safe for intravenous delivery. As well, the other in vitro characterization of the optimal nanoemulsion such as viscosity, percent transmittance, physical stability, and solubility study revealed it to be promising as an intravenous drug delivery system.

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Section: Introductionmentioning

confidence: 99%

Optimization of Olive Oil-Based Nanoemulsion Preparation for Intravenous Drug Delivery

2018

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Evaluation of testosterone compatibility with different excipients for the development of a self-emulsifying drug delivery system

Ribeiro

Cintra²,

Lima³

et al. 2022

J Therm Anal Calorim

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Solid Self-Emulsifying Drug Delivery System (Solid SEDDS) for Testosterone Undecanoate: In Vitro and In Vivo Evaluation

Liang¹,

Hua²,

Liu³

et al. 2021

CDD

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Objective: The current study aimed to investigate the potential of solid self-emulsifying drug delivery systems (solid SEDDS) loaded with testosterone undecanoate (TU) (solid TU-SEDDS). The solid TU-SEDDS was composed of TU, medium-chain triglycerides (MCT, oil), 2-Chloro-1-(chloromethyl) ethyl carbamate (EL-35, surfactant) and polyethylene glycol (PEG400, cosurfactant). It was expected to improve the dissolution and oral bioavailability of TU, as a result of investigating the feasibility of clinical application of SEDDS. Methods: First, a TU-SEDDS was developed by using rational blends of components with good solubilizing ability for TU. Next, a ternary phase diagram was constructed to determine the self-emulsifying region, and the formulation was optimized. Then, the solid TU-SEDDS formulation was established by screening suitable solid adsorptions. Finally, the prepared SEDDS, TU-SEDDS and solid TU-SEDDS formulations were evaluated in vitro and in vivo. Results: The size of the solid TU-SEDDS was 189.1 ± 0.23 nm. The transmission electron microscopy (TEM) results showed that the oil droplets were homogenous and spherical with good integrity. The differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) results indicated that the solid TU-SEDDS formulation almost preserves the amorphous state. Scanning electron microscopy (SEM) indicated that neusilin US2 successfully adsorbed the TU-SEDDS. Drug release indicated that the dissolution of the solid TU-SEDDS was faster than that of Andriol Testocaps®. Furthermore, in vivo pharmacokinetic (PK) studies in Sprague-Dawley (SD) rats showed that the area under the curve (AUC) of the solid TU-SEDDS (487.54±208.80 µg/L×h) was higher than that of Andriol Testocaps® (418.93±273.52 µg/L×h, P < 0.05). In beagles not fed a high-fat diet, the AUC of the solid TU-SEDDS (5.81±4.03 µg/L×h) was higher than that of Andriol Testocaps® (5.53±3.43 µg/L×h, P > 0.05). In beagles fed a high-fat diet, the AUC of the solid TU-SEDDS (38.18±21.90 µg/L×h) was higher than that of Andriol Testocaps® (37.17±13.79 µg/L×h, P > 0.05). Conclusion: According to the results of this research, oral solid TU-SEDDS is expected to be another alternative delivery system for the late-onset hypogonadism. This is beneficial to the transformation of existing drug delivery systems into preclinical and clinical studies.

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Solidification of Nanostructured Lipid Carriers Loaded Testosterone Undecanoate: In Vivo and In Vitro Study

Cited by 3 publications

References 37 publications

Optimization of Olive Oil-Based Nanoemulsion Preparation for Intravenous Drug Delivery

Optimization of Olive Oil-Based Nanoemulsion Preparation for Intravenous Drug Delivery

Evaluation of testosterone compatibility with different excipients for the development of a self-emulsifying drug delivery system

Solid Self-Emulsifying Drug Delivery System (Solid SEDDS) for Testosterone Undecanoate: In Vitro and In Vivo Evaluation

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