جستجوی مقالات مرتبط با کلیدواژه « Transdermal » در نشریات گروه « پزشکی »

 The repositioning of previously approved drugs is occupying the researchers’ plans. Baclofen (Bac) was our candidate for its established neuroprotective capacity, with a proposal of efficient drug delivery as non-ionic surfactant-based nanovesicles (NISNV) formulae against mild repetitive traumatic brain injury (mRTBI) in rats, thus reducing the number of orally or injected medications, especially in severely comatose patients or pediatrics.

 A (23 ) factorial design was implemented for confining Bac-loaded NISNV formulae, where a bunch of variables were inspected. An in-vivo experiment was done to test the prepared formula’s efficacy transdermally. The following parameters were measured: brain expression of gamma amino butyric acid B (GABAB), protein kinase C- α (PKC-α), focal adhesion kinase (FAK), TNF-α and nuclear factor kappa B (NF-κB) p65, malondialdehyde (MDA), superoxide dismutase (SOD), and histopathology.

 The particle size (PS) and entrapment efficiency percent (EE%) speckled from 60.40±0.28% to 88.02±0.01% for the former and 174.64±0.93 to 1174.50±3.54 nm for the latter. In vitro release% after 8 hours ranged from 63.25±5.47% to 84.79±3.75%. The optimized formula (F4) illustrated desirability=1, with 630.09±3.53 µg/cm2 of Bac permeated over 8 hours, which equates to 100% of Bac. Bac post-trauma treatment restored brain expression of GABAB and PKC-α, while decreasing FAK. Besides enhancing the histological findings, the anti-inflammatory effect was clear by decreasing TNF-α and NF-κB p65. Consequently, significant antioxidant sequelae were revealed herein by diminishing MDA levels and restoring SOD activity.

 Transdermal delivery of Bac-loaded niosomes confirmed neuroprotection and succeeded in surpassing skin-to-brain barriers, which makes it a promising therapeutic option for repeated traumas.

The skin is the body’s largest organ and serves as a site of administration for various medications. Transdermal drug delivery systems have several advantages over traditional delivery systems. It has both local and systemic therapeutic properties. Controlled plasma drug levels, reduced dosing frequency, and avoidance of hepatic first-pass metabolism are just a few of these systems’ advantages. To achieve maximum efficacy, it is critical to understand the kinetics, physiochemical properties of the drug moiety, and drug transport route. This manuscript focused on the principles of various physical means to facilitate transdermal drug delivery. Some examples are iontophoresis, electrophoresis, photomechanical waves, ultrasound, needleless injections, and microneedles. Mechanical, chemical, magnetic, and electrical energy are all used in physical methods. A major advantage of physical methods is their capability to abbreviate pain, which can be used for effective disease management. Further investigation should be carried out at the clinical level to understand these methods for effective drug delivery.

Diabetic somatic neuropathy is one of the most prevalent complications in type 1diabetes mellitus (T1D). Many treatments were investigated to alleviate the pain associatedwith this condition. Capsaicin is a naturally occurring lipophilic alkaloid that proved to be aneffective and safe treatment of chronic painful disorders. Despite the known therapeutic benefitsof capsaicin, the conventional topical formulations have limited bioavailability. Therefore, thecurrent study aims to develop capsaicin nanoemulgel to increase skin permeation and enhanceits activity against neuropathic pain.

Low-energy emulsification method was used to prepare nanoemulsions, usingeucalyptus oil as the oily phase, Tween 80 as a surfactant, propylene glycol, ethanol andisopropyl alcohol as co-surfactants. Pseudo-ternary phase diagrams were constructed toinvestigate and optimize the formulation. Subsequently, the optimum formulation wasformulated as a nanoemulgel and investigated for, skin permeation using Franz diffusion cell,and diabetic neuropathy (DN) management using alloxan-induced diabetic mice.

The selected nanoemulsion containing 0.05% capsaicin is composed of 8 % oil,24 % Smix (Tween 80: isopropyl alcohol 2:1 w/w) and 68 % water. It is characterized bynanosized globules (28.15 ± 0.24 nm) with a relatively low polydispersity index (0.27 ± 0.05).The nanoemulgel revealed circa 4-fold increase in capsaicin cumulative permeation whencompared to the conventional gel, and an improvement in its antinociceptive properties wasobserved in the treated diabetic mice (P < 0.05).

The selected capsaicin nanoemulgel would be a promising transdermal formulationthat may alleviate diabetic neuropathy in T1D patients.

Transdermal delivery over the past decade has become the field of interest for drug delivery due to its various advantages such as no first-pass metabolism, increased drug bioavailability, and easy administration. Different vesicle systems like ethosomes, liposomes, niosomes, and transferosomes along with particle systems like lipid nanoparticles, polymeric nanoparticles, carbon nanotubes, and fullerenes have been developed. These vesicles and particle systems have been developed using various easy and effective methods like cold injection method, rotary film evaporation, thin film hydration, high shear homogenization, solvent extraction method, and many more. These drug delivery systems are a very effective and feasible option for transdermal drug delivery and further developments can be made to increase their use. This article explains in detail the preparation methods and applications for these drug delivery systems.

Hydrophilic drugs are extensively applied in clinical applications. Inadequate dermal penetration of these drugs is a great challenge. Incorporation of drugs into nano-carrier systems overcomes lower penetration drawbacks. Invasomes are novel nano-carrier systems which enhance transdermal penetration by using terpene and ethanol in their structures. buprenorphine and bupivacaine hydrochlorides are two potent analgesic drugs that are loaded simultaneously in the nano-invasome structure as opioid and non-opioid drugs.

The full factorial experimental design was used for planning and estimating optimum formulations of invasome systems. Three influential factors like terpene type, terpene concentration and preparation method were comprehensively analyzed for achieving high encapsulation efficiency and optimum size.

The mean sizes of designed invasomes were in the range of 0.39-5.86 µm and high values of EE and LC were reported as 98.77 and 19.75 for buprenorphine-loaded invasome, respectively. Zeta potential measurements confirmed that the obtained high value of EE might be as a result of reversible ionic interactions between positively charged drugs and negatively charged phospholipidic part of invasome structure. Another characterization of the prepared formulations was carried out by FTIR, XRD and DLS technique.

The satisfactory obtained results of formulations encourage researchers to get optimum topical analgesic formulations with potent and rapid onset time properties required in invasive cutaneous procedures.

The objective of the current study was to develop Ibuprofen (IBP) gel using different polymers individually and in combination and then to select best gel formulation based on various in-vitro evaluation parameters such as bioadhesive strength, gel strength, spreadability, viscosity and drug release study. The selected gel formulation was found to be composed of 1% (w/w) each of hydroxypropyl methylcellulose (HPMC K100M) and sodium carboxy methylcellulose (NaCMC). Two techniques such as chemical method using 1,8-cineole as chemical penetration enhancer (CPE) and physical technique using microneedle were employed to improve IBP permeation across the abdominal skin of rat. Out of the two techniques, the later technique showed higher (2.865-fold) permeation enhancement compared to control. Furthermore, a synergistic effect was also observed when both the techniques were used simultaneously with 3.307-fold increase in permeation enhancement. In-vivo anti-inflammatory study on rats induced with carrageenan paw oedema and analgesic activity investigation by tail flick method in rat model exhibited sustained effect up to 8 h compared to orally treated group. The stability study at room and accelerated conditions for three months did not show any sign of instability. Thus, the developed IBP gel is stable and have potential to illicit both anti-inflammatory and analgesic effect when administered transdermally.

The aim of the present study was to characterize and evaluate the nanoemulgel (NEG) of snakehead fish powder (SFP), as a transdermal delivery system for poorly water soluble drug, in order to conquer the inconveniences related to its oral conveyance. Diverse nanoemulsion components (oil, surfactant, and co-surfactant) were chosen based on solvency and emulsification capacity. SFP loaded nanoemulsion which tested by stress-stability testing was carried out for all formulations and those that passed these tests were characterized for mean droplet size, polydispersity index (PDI), zeta potential, pH, viscosity, and transmittance. After that, this was continued by permeation studies using snake skin in vitro and rabbit skin in vivo studies i.e. skin irritation study and the effectiveness test. Mean droplet size and zeta potential of the optimized nanoemulsion (NE4) were found to be 98.6 ± 0.93 nm (polydispersity index, PDI = 0.1 ± 0.20) and -57.5 ± 0.3 mV respectively. Optimized nanoemulsion was converted into nanoemulgel with 1.5% w/v of gelling agent (HPMC) and evaluated for pH, viscosity, spreadability, and extrudability measurement. Ex vivo transdermal permeation value for SFP through snake skin as membrane from NEG1, NEG2, NEG3 and marketed SFP cream showed results of 55.65 ± 0.93%, 56.14 ± 0.70%, 66.75 ± 1.03% and 49.80 ± 3.42% respectively in 3 hours. Moreover, all the treatment group did not show skin irritation of each group. The effect of burn wound healing of NEG3 showed a significant (P<0.05) on the measurement of wound area compared to marketed cream. The novel NEG of SFP was successfully formulated for transdermal application based on the results of evaluations and stability tests on accelerating burn wound healing.

Since two decades or so transdermal route established itself as better alternative to traditional oral route. This is possible due to continuous innovations in transdermal drug delivery (TDD), which not only enables researchers from academia and industry to successfully develop and launch many new pharmaceuticals but also allow to include new classes of drugs that can be developed into transdermal formulations. These successes are achieved due to the use of novel techniques based on either physical or chemical approaches. However, both of these techniques suffer due to their own disadvantages. Comparatively, a simple method of supersaturation to enhance drug permeation across skin has created a new wave of interest. Even though the application supersaturated principle in topical and TDD has been used from 1960s, but proper control of drug release and formation of stable supersaturated states has been the core of intense research in the last decade. Out of various methods used to get supersaturated system, evaporation method is considered as most efficient and practically feasible for TDD. Therefore, in this review concept of supersaturation, selection of solvent system and the mechanism of inhibition of crystallization are discussed. Application of evaporation systems in the development of transdermal formulations such as solutions, semisolids and metered dose therapeutic systems (MDTS) and the commercial evaporative systems are also discussed in this review.

Ofloxacin is a fluoroquinolone with broad-spectrum antibacterial action, used in treatment of systemic and local infections. Ofloxacin is BCS class II drug having low solubility, high permeability with short half-life. The present work was aimed to design, develop and optimize gellified emulsion of Ofloxacin to provide site targeted drug delivery. Transdermal drug delivery will enhance the bioavailability of the drug giving controlled drug release.
Transdermal drug delivery system was designed with gelling agent (Carbopol 940 and HPMC K100M), oil phase (oleic acid) and emulsifying agent (Tween 80: Span 80). Effect of concentration of gelling agent on release of drug from transdermal delivery was studied by 32 factorial design. Emulgel was evaluated for physical appearance, pH, drug content, viscosity, spreadability, antimicrobial activity, in- vitro diffusion study and ex-vivo diffusion study.
FE-SEM study of the emulsion batch B5 has revealed formation of emulsion globules of approximately size 6-8 µm with -11.2 mV zeta potential showing good stability for the emulsion. Carbopol 940 had shown greater linear effect on drug release and viscosity of the formulations due to its high degree of gelling. In-vitro diffusion study through egg membrane had shown 88.58±1.82 % drug release for optimized batch F4. Exvivo diffusion study through goat skin indicated 76.68 ± 2.52% drug release.
Controlled release Ofloxacin emulgel exhibiting good in-vitro and ex-vivo drug release proving good antimicrobial property was formulated.

Conventional transdermal drug delivery systems (TDDS) have been designed for drug delivery through the skin. These systems use the permeability property of stratum corneum, the outermost surface layer of the skin. Applying polymeric micro and nanofibers in drug delivery has recently attracted great attention and the electrospinning technique is the preferred method for polymeric micro-nanofibers fabrication with a great potential for drug delivery. More studies in the field of nanofibers containing drug are divided two categories: first, preparation and characterization of nanofibers containing drug and second, investigation of their therapeutic applications. Drugs used in electrospun nanofibers can be categorized into three main groups, including antibiotics and antimicrobial agents, anti-inflammatory agents and vitamins with therapeutic applications. In this paper, we review the application of electrospun polymeric scaffolds in TDDS and also introduce several pharmaceutical and therapeutic agents which have been used in polymer nanofibrous patches.

Due to its minimal systematic adverse effects, transdermal estrogen is widely used for the prevention of osteoporosis in postmenopausal women.The present meta-analysis aimed to clarify the effects of transdermal estrogen on bone mineral density (BMD) of postmenopausal women.
Studies were identified by searching electronic databases including Cochrane Library, MEDLINE, Embase, and CINAHL databases, and the Sciences Citation Index. Systematic review of articles published between January 1989 to February 2016.Reference lists of the included articles were also evaluated and consultations were made with relevant experts. While 132 studies included the desired keywords, only nine clinical trials met the inclusion criteria and were finally reviewed.
Main The pooled percent change in BMD was statistically significant in favor of transdermal estrogen. According to the resulting pooled estimate, lumbar spine BMD one and two years after transdermal estrogen therapy was respectively 3.4% (95% CI: 1.7-5.1) and 3.7% (95% CI: 1.7-5.7) higher than the baseline values. The test for heterogeneity was not statistically significant based on the I2 heterogeneity index.
One-two years of transdermal estrogen delivery can effectively increase BMD and protect the bone structure in postmenopausal women.

The aim of the present study was to develop and investigate the feasibility of delivering Nebivolol as a transdermal patch by iontophoresis. The passive and electrically assisted transdermal delivery of Nebivolol hydrochloride by iontophoresis will improve the therapeutic efficacy and overcome the difficulties raised in oral drug delivery. Because of its extensive hepatic metabolism and low dose, Nebivolol hydrochloride become a suitable candidate for transdermal administration. The matrix transdermal patches of Nebivolol hydrochloride were prepared and tested for in-vitro drug release and ex-vivo permeation. The study was conducted with the help of silver-silver chloride electrodes by iontophoresis across hairless rat skin. Drug release was evaluated in the presence of iontophoresis field using a current density of 0.5 mA/cm2 or without electric field i.e passive diffusion by the process of electro-migration and electro-osmosis. Drug was measured spectrophotometrically and flux was determined. The flux of Nebivolol significantly increased (P<0.05) with increase in current strength from 0.5 – 1.0 mA/cm2. The findings show that Nebivolol hydrochloride matrix transdermal therapeutic systems could be prepared with the required flux having suitable mechanical properties. It can be concluded from the results that the appliance of iontophoresis with penetration enhancer enhances the flux compared to the passive diffusion.

Celecoxib is a selective cyclo-oxygenase-2 inhibitor recommended orally to treat arthritis and osteoarthritis. It is a highly lipophilic, poorly soluble drug with oral bioavailability of around 40%. Long term oral administration of celecoxib causes serious gastrointestinal side effects.. The current study aimed to assess the skin permeation of celecoxib by a transdermally applied liposomal formulation.. Liposomes were prepared by thin film method using soya lecithin and cholesterol. Physicochemical characteristics of the liposomes such as, particle size, drug encapsulation efficiency were determined. Also, drug release and in vitro skin permeability through rat skin were evaluated using Franz diffusion cells.. The results showed that the maximum drug encapsulation efficiency was 43.24%. Drug release profile showed that 81.25% of the drugs released in the first 24 hours of the experiment. Fluxes (Jss), permeability coefficient (P), diffusivity coefficient (D) parameters of the optimum liposomal formulation were significantly higher than those of saturated aqueous solution of celecoxib. The decrease of lecithin increased values. Particle sizes of the formulations ranged from 0.117 to 1.123 µm. Jss, Dapp and P parameters in L - 8 formulations were 29.18, 60.95, and 3.21 times higher than those of saturated water solution of celecoxib, respectively. The results of vesicles characterization indicated the potential application of celecoxib loaded liposome as carrier system.. In conclusion, the components such as lecithin and cholesterol, and vortex time in liposomal formulations have an essential role in the physicochemical properties and celecoxib permeability through rat skin..

purpose of the present study was to explore the passive and electrically assisted transdermal transport of Granisetron hydrochloride (GRA) in solution and gel formulation through iontophoresis and also the feasibility of delivering therapeutic amounts of drug for the treatment of chemotherapy-induced nausea and vomiting. In this study, iontophoretic permeation of GRA through guinea pig skin using silver-silver chloride electrode was performed and the effects of different variables on this phenomenon were evaluated. Preliminary in-vitro studies using aqueous GRA formulations investigating the effect of drug concentration (5, 10, 15 and 20 mg mL-1) on passive permeation, current density (0.2, 0.4 and 0.5 mA cm-2), mode of current application, penetration enhancers and effect of application duration were performed. As expected, GRA delivery was found to be increased with the elevation in drug concentration and current density. Anodal continuous current delivery was more effective in the permeation of GRA than the pulsed current method. Penetration enhancers were ineffective to show synergistic effect in conjunction with iontophoresis. It was evident that reservoir in the skin was not formed during the iontophoretic delivery. The results confirm that GRA is an excellent candidate for iontophoresis. The present study demonstrated the feasibility of GRA transdermal transport through the Lutrol F-127 gel by iontophoresis. Further in-vivo studies will be required to support in-vitro conclusions and develop in-vitro, in-vivo correlations.

Topical drug dosage forms such as ointments and creams can be easily removed through wetting, movement and contact. The new bioadhesive formulations with enhanced local anesthetic effects are needed for topical administration. The adhesive capacity of hydroxypropyl methylcellulose (HPMC) was determined by measuring the maximum detachment force and the adhesion work with an auto peeling tester. The release of drug from a HPMC gel was studied according to the drug concentration. Permeation study through the rat skin was performed at 37°C using phosphate buffer solution (pH = 7.4) as a receptor medium. To increase the skin permeation of bupivacaine from the HPMC gels, penetration enhancer such as the saturated and unsaturated fatty acids, the pyrrolidones, the propylene glycol derivatives, the glycerides, and the non-ionic surfactants were incorporated in the bupivacaine-HPMC gels. The local anesthetic effect of the formulated gel preparation was examined using a tail-flick analgesimeter. As the concentration of HPMC increased, the bioadhesive force and viscosity were increased. The rate of drug release was increased with increasing the drug concentration. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the most enhancing effects on drug permeation through the skin. In the rat tail flick test, the area under the efficacy curve of bupivacaine gel containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed a 2.36-fold increase in anesthetic activity compared to control gel without any additives. The bupivacaine gels containing both penetration enhancer and vasoconstrictor showed enhancement and prolonged efficacy compared to the control gel. To enhance the local anesthetic effects of bupivacaine, the transdermal bupivacaine gel formulation containing penetration enhancer and vasoconstrictor could be developed.

Topical and transdermal drug delivery systems are noninvasive and can be self-administered with the minimization of side-effects, have received increased attention during the past few years. Nanoemulsions, emulsions sized between 20-200 nm with narrow distributions, offer several advantages for topical and transdermal delivery of pharmaceutical agents including controlled droplet size, the ability to efficiently dissolve lipophilic drugs, enhanced skin permeation and extended release of lipophilic and hydrophilic drugs. Moreover, they exert good sensorial and physical properties such as complete dispersion on skin and skin hydration in cosmetic products. The review deals with nanoemulsion applications in topical and transdermal drug and gene delivery.