Cambios bioquímicos en el tejido cavernoso causados por resección unilateral del nervio cavernoso y efectos del ácido alfalipoico en estos cambios

Alan, Cabir; Koçoğlu, Hasan; Ersay, Ahmet Reşit; Kurt, Hasan; Ertung, Yunus; Alan, Hale

doi:10.1016/j.acuro.2010.03.034

Cited by 3 publications

(2 citation statements)

References 21 publications

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“…Alpha-lipoic acid (ALA) is a powerful antioxidant that is also known as acetate replacing factor. ALA improves sexual function and used in the treatment of diabetic impotence due to its antioxidant activity 19–23. Recently, ALA has been used as a formulation excipient to improve the delivery and efficacy of drugs 24,25…”

Section: Introductionmentioning

confidence: 99%

<p>Zein-alpha lipoic acid-loaded nanoparticles to enhance the oral bioavailability of dapoxetine: optimization and clinical pharmacokinetic evaluation</p>

El-Say¹,

Ahmed²,

Mohamed³

et al. 2019

IJN

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BackgroundPremature ejaculation (PE) is the most common type of male sexual disorder with important psychological consequences. Dapoxetine (DPX), a recently approved drug for the treatment of PE, suffers from low bioavailability with large variability that ranges from 15–76% (mean 42%) after oral administration. The objective of this study is to optimize the parameters for the preparation of DPX-Zein-alpha lipoic acid (ALA) nanoparticles (NPs) to improve the bioavailability of DPX and consequently decrease therapeutic dose and adverse effect, leading to patient satisfaction and compliance.MethodsWe investigated the effect of ALA concentration, PVA concentration and stirring rate on nanoparticle size (Y1), zeta potential (Y2), initial DPX release (Y3) and cumulative DPX release (Y4). In addition, in vivo pharmacokinetic study was performed for the optimized DPX formulation on human healthy volunteers compared with marketed DPX tablet.ResultsThe optimized DPX-loaded NPs showed Y1, Y2, Y3, and Y4 of 159.24 nm, 19.14 mV, 25.31% and 95.9 %, respectively. A single oral dose of 30 mg of optimized DPX-loaded NPs to human volunteers resulted in 2-fold improvement of AUC (1376.145±339.592 vs 709.178±146.307 in DPX), 4-fold increase in tmax (2.5±0.314 vs 0.583±0.144), prolongation of MRT (7.637±1.373 compared to 6.031±1.826 h), but with reduction in t1/2 (5.283±1.077 vs 8.452±2.813).ConclusionThe clinical findings suggest 194% enhancement of relative bioavailability of the optimized DPX-loaded NPs, potentially leading to a decrease in therapeutic dose and associated side effects in the treatment of PE.

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Section: Introductionmentioning

confidence: 99%

<p>Zein-alpha lipoic acid-loaded nanoparticles to enhance the oral bioavailability of dapoxetine: optimization and clinical pharmacokinetic evaluation</p>

El-Say¹,

Ahmed²,

Mohamed³

et al. 2019

IJN

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“…ALA has shown significant improved sexual function and quality of life in both animals and human investigations 6 – 9 . Previous reports showed the potential use of ALA in the treatment of diabetic impotence through prevention of corpus cavernosum dysfunction 10 , 11 .…”

Section: Introductionmentioning

confidence: 99%

Development and single dose clinical pharmacokinetics investigation of novel zein assisted- alpha lipoic acid nanoencapsulation of vardenafil

Ahmed

2018

Sci Rep

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The aim of this study was to utilize the biocompatibility of the natural ingredients zein and alpha lipoic acid (ALA) as a novel nanosphere matrix formulation that encapsulates vardenafil (VRD) for improved drug delivery and bioavailability. Three formulations were prepared using zein: ALA ratio of 1:1, 2:1 and 3:1 by liquid–liquid phase separation method. Physicochemical characterization and in vitro diffusion evaluation were carried out for the prepared formulations. A single dose clinical pharmacokinetic study was carried out for the selected formulation. Results revealed VRD formulations showed particle size of 836.7 ± 191.3, 179.8 ± 18.4 and 147.3 ± 18.1 nm and encapsulation efficiency of 55.72 ± 4.36, 65.33 ± 7.82 and 69.38 ± 6.83% for F1, F2 and F3, respectively. Single dose clinical pharmacokinetic results, in healthy human volunteers, showed improved VRD bioavailability by 2.5 folds from nanosphere formula (F3) compared with the marketed tablets. The formulation of novel zein-ALA nanospheres offers the possibility for application of a biocompatible nano-carrier system in drug delivery for improved drug delivery and efficacy.

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Role of oxidative stress in surgical cavernous nerve injury in a rat model

Wang

Ding

et al. 2015

J of Neuroscience Research

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This study investigates the role of oxidative stress in surgical cavernous nerve (CN) injury in a rat model. Eighty-four male Sprague-Dawley rats were randomly divided into three groups: group 1, sham-operated rats; group 2, bilateral CN-crushed rats; and group 3, bilateral CN-transection-and-sutured-immediately rats. Oxidative stress was evaluated by malondialdehyde levels, super oxide dismutase (SOD) activities, and glutathione peroxidase (GPX) activities in serum. Erectile function was assessed by CN electrostimulation at 3 months with mean maximal intracavernous pressure (ICP) and maximal ICP per mean arterial pressure. Nerve injury was assessed by toluidine blue staining of CNs and nicotinamide adenine dinucleotide phosphate (NADPH)-diaphorase staining of penile tissue. GPX protein expression and nitrotyrosine-3 (NT-3) levels in penile tissue were measured. Erectile function and the number of myelinated axons of CNs and NADPH-diaphorase-positive nerve fibers were statistically decreased between groups, from sham to crush to transection. For markers, both nerve-injury groups showed increased oxidative stress markers at early time points, with the transection group showing greater oxidative stress than the crushed group and values normalizing to sham levels by week 12. GPX expression and NT-3 levels in penile tissue were in concordance with the results of SOD and GPX. These results show that oxidative stress plays an important role in injured CNs, and different methods of CN injury can lead to different degrees of oxidative stress in a rat model.

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Cambios bioquímicos en el tejido cavernoso causados por resección unilateral del nervio cavernoso y efectos del ácido alfalipoico en estos cambios

Cited by 3 publications

References 21 publications

<p>Zein-alpha lipoic acid-loaded nanoparticles to enhance the oral bioavailability of dapoxetine: optimization and clinical pharmacokinetic evaluation</p>

<p>Zein-alpha lipoic acid-loaded nanoparticles to enhance the oral bioavailability of dapoxetine: optimization and clinical pharmacokinetic evaluation</p>

Development and single dose clinical pharmacokinetics investigation of novel zein assisted- alpha lipoic acid nanoencapsulation of vardenafil

Role of oxidative stress in surgical cavernous nerve injury in a rat model

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