Feasibility of binary composition in development of nanoethosomal glycolic vesicles of triamcinolone acetonide using Box-behnken design: in vitro and ex vivo characterization (original) (raw)

Feasibility of binary composition in development of nanoethosomal glycolic vesicles of triamcinolone acetonide using Box-behnken design: in vitro and ex vivo characterization View supplementary material

Artificial Cells, Nanomedicine, and Biotechnology, 2016

Triamcinolone acetonide (TA) employed for the treatment of atopic dermatitis exhibits limited penetration into the epidermis. This investigation aimed to explore the role of binary solvents in topical drug delivery of TA by developing nanoethosomal glycolic lipid vesicles by infusion method. Screening of vesicles (TA1-TA17) formulated by Box Behnken design identified the optimized formulation (TA10) that was developed as carbomer gels. The gels were then evaluated for pharmaceutical properties and compared with control and reference ethosomal gel (RG). Higher in vitro permeation was found in gels containing TA10, prepared with or without using penetration enhancer (EGP 83.76 ± 0.72% and EG 82.42 ± 0.89%, respectively). CLSM studies depicted deeper uniform penetration of fluorescent tracer into the epidermis via EG as compared with RG and control gel. Enhanced penetration was due to combinational solvent effect exerted by ethanol and propylene glycol. Histological analysis confirmed the nonirritant potential of the gel. Thus, it can be concluded that nanoethosomal glycolic vesicles proved to be an effective non irritant carrier for improvised penetration of triamcinolone acetonide for potential topical therapeutics.

Formulation and in vitro Evaluation of Topical Liposomal Gel of Triamcinolone Acetonide

2013

Triamcinolone acetonide is a glucocorticoid that it is used in treatment of skin inflammatory diseases. liposomes can increase the deposition of drugs within the skin at the site of action and reduce side effects of drug. The aim of the present study was to formulate and evaluate liposomal vesicles loaded with triamcinolone acetonide. liposomes containing triamcinolone acetonide were prepared using thin film method. The quantities of lecithin and cholesterol were changed to enhance the encapsulation of the drug. Carbomer 940 was used as gel base and four different gel formulations including hydroalcoholic gel, MLV liposomal gel, SUV liposomal gel and blank MLV gel containing free drug were prepared. The release profile of triamcinolone acetonide was determined using dialysis membrane method. Liposomes were also characterized by optical microscope and their particle size was also determined. Formulation containing lecithin: drug: cholesterol (100: 10: 10) having about 90.05 percent encapsulation was selected as the best formulation and the results of release showed SUV liposomal gel has the most regular and the least interaction between the drug and polymer. Results of particle size determination showed 50% of MLV and SUV liposomes had diameter below 33.80 μm and 22.09 μm, respectively. The results of characterization of the vesicles indicated the potential application of triamcinolone acetonide loaded liposome as carrier system.

DEVELOPMENT OF LIPID-BASED VESICLES OF TERBINAFINE GEL FOR SKIN DELIVERY BY 3 2 FULL FACTORIAL DESIGN

International Journal of Applied Pharmaceutics, 2024

Objective: Terbinafine is a poorly water-soluble and highly permeable allylamine antifungal (BCS-II) drug. In this study, we looked at the possibility of using ethosomes as vesicular lipid nanocarriers to enhance the transdermal delivery of terbinafine. Methods: Using a 3 2 full factorial design, the ethosomal formulation with different soya lecithin and cholesterol concentrations was improved and optimized. The influence of independent variables, namely soya lecithin and cholesterol concentration in ethosomes was determined by estimating dependent variable including the particle size, polydispersity index, zeta potential, entrapment efficiency, and in vitro drug release. To improve the residence time of ethosomes on the topical application, the ethosomes were incorporated into the carbopol gel. 1% w/v of Carbopol 934 P gelembedded Terbinafine ethosomes were used to study medication release and skin interactions. Results: Optimized ratios of soya lecithin and cholestrol was used to prepare vesicles. Formulation had a particle size of 1207.39±2.71 nm, entrapment efficiency of 94.46±0.47%, and in vitro diffusion of 51.27±0.16%. It was found that the growth of fungus Aspergillus niger and Candida albicans were inhibited by Ethosomal Gel. However, ethosomal gel had more inhibitory activity on Apergillus niger compared to positive control. Conclusion: The current study suggests that ethosomal vesicles may improve transdermal dispersion without causing skin irritation. Terbinafineloaded ethosomes have the potential to be one of the most important transdermal application techniques for the treatment of fungi-related disorders.

Recent Advances in Lipid-Based Vesicles and Particulate Carriers for Topical and Transdermal Application

Keywords: liposomes nanoparticles drug delivery systems transdermal drug delivery permeability percutaneous controlled release colloid skin lipids a b s t r a c t In the recent decade, skin delivery (topical and transdermal) has gained an unprecedented popularity, especially due to increased incidences of chronic skin diseases, demand for targeted and patient compliant delivery, and interest in life cycle management strategies among pharmaceutical companies. Literature review of recent publications indicates that among various skin delivery systems, lipid-based delivery systems (vesicular carriers and lipid particulate systems) have been the most successful. Ve-sicular carriers consist of liposomes, ultradeformable liposomes, and ethosomes, while lipid particulate systems consist of lipospheres, solid lipid nanoparticles, and nanostructured lipid carriers. These systems can increase the skin drug transport by improving drug solubilization in the formulation, drug partitioning into the skin, and fluidizing skin lipids. Considering that lipid-based delivery systems are regarded as safe and efficient, they are proving to be an attractive delivery strategy for the pharmaceutical as well as cosmeceutical drug substances. However, development of these delivery systems requires comprehensive understanding of physicochemical characteristics of drug and delivery carriers, formulation and process variables, mechanism of skin delivery, recent technological advancements, specific limitations, and regulatory considerations. Therefore, this review article encompasses recent research advances addressing the aforementioned issues.

FORMULATION DEVELOPMENT AND CHARACTERIZATION OF TRIAMCINOLONE LOADED CUBOSOMES FOR TRANSDERMAL DRUG DELIVERY

IJPSM, 2021

Psoriasis is a chronic condition that is caused by the negative signals given by immune system, which leads to hyperproliferation and other inflammatory reactions on the skin. These conditions may adversely affect the quality of the patient's life leading to psychological stress. Topical delivery of drug is always preferred for Psoriasis because other treatments may lead to systemic intoxication and other adverse reactions. Triamcinolone is a topical corticosteroid belonging to BCS class IV (low solubility and permeability) used to treat Psoriasis. The limitations with transdermal delivery is that only a small amount of the drug can be transferred through the skin tissue due to the barrier effects of the Stratum corneum. Therefore, Novel transdermal delivery system, Cubosomes belonging to Nanostructured lipid carriers were chosen to overcome the issues of solubility and permeability. Twelve formulations were prepared with various ratios of Glyceryl monooleate (2.5 to 5%) & Poloxamer 407 (0.5 to 2%) and the formulations were evaluated for particle size, PDI, zeta potential, entrapment efficacy, drug content and in-vitro release. The best composition of Cubosomes was selected and incorporated into transdermal patch and the formulated patches were evaluated.

Passive Enhancement of Transdermal Drug Delivery: Lipid-Based Colloidal Carriers as an Emerging Pharmaceutical Technology Platform

2019

Transdermal drug delivery (TDD) is an attractive approach to minimize the limitations encountered by other drug administration routes such as oral and parenteral. Apart from specialized devices fabricated for modifying the barrier properties of the stratum corneum such as iontophoresis, sonophoresis and microneedles, there are several passive methods applied through physicochemical manipulations in drug formulation, including prodrugs, ion-pairs, supersaturated solutions, inclusion complexes, eutectic mixtures, ionic liquids and use of chemical penetration enhancers. More recently, colloidal carriers due to their small size, high specific surface area, unique structural and biochemical features, are suggested for the skin penetration enhancement through transcellular or shunt routes. This review considers challenges and achievements of colloidal TDD systems, either used alone or in combination with other techniques, with a special concern about lipid-based vesicular nanocarriers inc...

Novel vesicular carriers for topical drug delivery and their applications

International Journal of Pharmaceutical Sciences Review and Research

Delivery of drug through topical route represents a most convenient and novel approach. The major difficulty arises while delivering a drug through skin is its action as a natural barrier nature which makes it difficult for most drugs to penetrate into and permeate through it. Conventional topical formulations have not proved to be effective in dermal delivery of drug. Novel drug delivery systems bear great potential for dermal delivery. Among them lipidic and non-lipidic vesicular systems like liposome, noisome, transfersome and ethosome have been suggested to overcome the problems associated with conventional topical formulations. These vesicular systems were found to be more effective as they render controlled release of drug due to depot formation in skin and some were more effective in transdermal delivery. This article summarizes the potential of novel vesicular drug delivery carrier based dermal applications of the drug.

Benchmark in the era of drug carriers for semisolid based topical delivery system

A liposome is a microscopic vesicle consisting of an aqueous core enclosed in one or more phospholipid layers, used to convey vaccines, drugs, enzymes, or other substances to target cells or organs. Liposomes are bilayered structures made of amphipathic (both hydrophobic and hydrophilic) phospholipids/cholesterol that spontaneously form closed structures when hydrated in aqueous solutions. Liposomes are acceptable and superior carriers having ability to encapsulate hydrophilic and lipophilic drugs and protect them from degradation. Topical liposomes have similarity to biological membranes they can store water-soluble and lipophilic substances in their different phases. Moreover, they are similar to the epidermis with respect to their lipid composition, which enables them to penetrate the epidermal barrier to a greater extent compared to other dosage forms. According to studies performed so far liposomes are biodegradable and non-toxic. The really new aspect with liposomes is that th...

In Situ Gel of Triamcinolone Acetonide-Loaded Solid Lipid Nanoparticles for Improved Topical Ocular Delivery: Tear Kinetics and Ocular Disposition Studies

Nanomaterials

Triamcinolone acetonide (TA), an intermediate acting corticosteroid, is used in the treatment of posterior ocular diseases, such as inflammation, posterior uveitis, and diabetic macular edema. The objective of this investigation was to prepare TA-loaded solid lipid nanoparticles (TA-SLNs) and in situ gel (TA-SLN-IG) formulations for delivery into the deeper ocular tissues through the topical route. TA-SLNs were prepared by hot homogenization and ultrasonication method using glyceryl monostearate and Compritol® 888ATO as solid lipids and Tween®80 and Pluronic® F-68 as surfactants. TA-SLNs were optimized and converted to TA-SLN-IG by the inclusion of gellan gum and evaluated for their rheological properties. In vitro transcorneal permeability and in vivo ocular distribution of the TA-SLNs and TA-SLN-IG were studied using isolated rabbit corneas and New Zealand albino rabbits, respectively, and compared with TA suspension, used as control (TA-C). Particle size, PDI, zeta potential, ass...

Formulation and evaluation of topical gel containing nanostructured lipid carriers dispersion of an antifungal drug

ACTA Pharmaceutica Sciencia, 2019

Fungal infection are the common dermatological diseases. Drug delivery systems for topical use have shown significant advantages in targeting the drug to the action site in the body and also reduces the systemic side effects. In the present study an attempt was made to prepare econazole nitrate loaded nanostructured lipid carrier (NLC). Different formulations were prepared by hot homogenization technique using solid lipid and liquid lipid (GMS, GMO) and surfactants (Poloxamer 188, Poloxamer 407). Formulations were characterized for entrapment efficiency, viscosity, spreadability, pH and in vitro drug release. Entrapment efficiency of formulation F1-F8 was found to be 65.81-74.63%. The drug release of NLC gel followed zero order kinetics. NLC gel were stable at 40 ± 2ֹ°C and 75 ± 5% RH. Thus, the prepared NLC gel proved to be a potential candidate as a topical nanoparticulate sustained drug delivery system for econazole nitrate.