Ethosomal Gel Research Articles

Revitalizing the local anesthetic effect of Mebeverine hydrochloride via encapsulation within ethosomal vesicular system

Mebeverine hydrochloride (MBH) is an antispasmodic drug that holds the potential to exert a local anesthetic action via blocking voltage operated sodium channels. However, its local anesthetic activity was not yet exploited due its poor skin permeability. Nanocarriers have emerged as efficient vehicles for delivering both lipophilic and hydrophilic drugs through the stratum corneum. In this study, therefore, the efficacy of ethosomes for delivering MBH via skin for local anesthetic effect was investigated. The ethosomes were formulated, optimized and characterized for particle size, zeta potential, entrapment efficiency and in vitro permeation studies. Then, the optimized formula was incorporated into Carbopol 940® gel and evaluated for skin irritation and in vivo local anesthetic action. Ethosomes were spherical in shape with vesicle sizes varied from 308.2 ± 18.2 nm to 78.8 ± 8.6 nm and entrapment efficiencies of 18–65%. In vitro drug permeation across rabbit ear skin revealed enhanced drug permeation and higher transdermal flux with ethosomal formulations, compared to aqueous drug solution. In addition, an ethosomal gel of optimized formula showed a potent local anesthetic effect as manifested by a 2.3-fold increase in the area under the efficacy curve (AUEC) of MBH loaded ethosomal gel, compared to the MBH gel. Furthermore, skin irritation experiments demonstrated that MBH ethosomal gel induced neither erythema nor edema upon application to rabbit skin. Collectively, MBH loaded ethosomal vesicles might represent a promising delivery vehicle for safe and efficient local anesthetic effect.

Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients.

To enhance anthralin efficacy against psoriasis and reduce its notorious side effects, it was loaded into various liposomal and ethosomal preparations. The nanocarriers were characterized for drug encapsulation efficiency, size, morphology and compatibility between various components. Optimum formulations were dispersed in various gel bases and drug release kinetics were studied. Clinical efficacy and safety of liposomal and ethosomal Pluronic®F-127 gels were evaluated in patients having psoriasis (clinicaltrials.gov identifier is NCT03348462). Safety was assessed by recording various adverse events. Drug encapsulation efficiency ≥97.2% and ≥77% were obtained for liposomes and ethosomes, respectively. Particle sizes of 116 to 199 nm and 146 to 381 nm were observed for liposomes and ethosomes, respectively. Fourier-Transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) studies confirmed the absence of interaction between anthralin and various nanocarrier components. Tested gel bases showed excellent ability to sustain drug release. At baseline, the patients had a median Psoriasis Area and Severity Index (PASI) of 3.4 for liposomes and 3.6 for ethosomes without significant difference. After treatment, mean PASI change was −68.66% and −81.84% for liposomes and ethosomes, respectively with a significant difference in favor of ethosomes. No adverse effects were detected in both groups. Anthralin ethosomes could be considered as a potential treatment of psoriasis.

Potential treatment of arthritis with an optimized Mometasone Furoate loaded-ethosomal gel in carrageenan-induced rat joint arthritis

The aim of this work was to improve the transdermal delivery of Mometasone Furoate (MF) by developing an optimal ethosomal system for targeting inflammatory cases. The effects of Phospholipon 90G (PC90G) (X1), ethanol (X2), propylene glycol (PG) (X3) and sonication time (X4) were optimized for their effects on entrapment efficiency (Y1), vesicle size (Y2), zeta potential (Y3), skin flux (Y4) and skin accumulation (Y5) using Box Behnken design. The optimal MF formula (OMF) was characterized and underwent a comparative skin penetration study with the liposomal system and hydroalcoholic dispersion of MF. OMF was loaded into Carbopol gel for conducting a comparative in-vivo study with standard MF loaded gel and the market product using a carrageenan-induced rat joint arthritis model. The observed values of OMF were 68.44%, 62.87 nm, −15.92 mV, 7.42 μg/cm2/h and 16.63 μg/cm2/24h for Y1, Y2, Y3, Y4, and Y5; respectively. X2 and X3 were the main factors affecting Y1, Y3, Y4 and Y5 while Y2 was mainly affected by sonication time. TEM images showed ethosomal vesicles with multiple layers of the spherical structure. The skin flux of OMF was 2.33 and 3.53 folds of liposomes, hydroalcoholic dispersion; respectively. Moreover, the confocal laser scanning microscopy (CLSM) confirmed the penetration potential of OMF over other systems. Daily application of ethosomal gel for ten days significantly improved the arthritis degree while normal joint histological structures were observed after twenty days. Therefore, MF-loaded ethosomes represents a promising therapeutic approach for the treatment of arthritis.

Development of Ethosomal Gel from Withania Somnifera

Novel drug delivery systems are used to increase administration of drugs through transdermal system. Ethosomes has the ability to permeate through the stratum corneum. Ethosomes are the delivery carriers that enable the drugs to reach the deep skin layers as well as the systemic circulation. These vesicles are well known for their importance in cellular communication and in particle transportation for many years. This article reviews various aspects of ethosomes which includes their preparation, characterization, advantages and their applications in drug delivery. Ethosomes has number of important benefits such as, it improves the drug’s efficacy, enhances the patient compliance, comfort and reduces the total cost of treatment.

Herbal ethosomal gel containing luliconazole for productive relevance in the field of biomedicine.

This study includes development, characterization, and optimization of herbal ethosomal formulation. The aim of the present study is to develop drug loaded ethosomes capped with Azadirachta indica (neem) which, was further incorporated in Carbopol 934K thereby, resulting in the formation of ethosomal gel. The formulation is aimed to express effective treatment against fungal infection. The build was formulated using drug (Luliconazole), soyalecithin, ethanolic neem extract and propylene glycol. In total nine ethosomal, formulations of distinct concentrations of ingredients were processed, to determine out the optimized formulation among the all. Further the prepared drug loaded ethosomes were subjected to various evaluation parameters like particle size, zeta potential, polydispersity index (PDI) and % entrapment efficiency. For the evaluation of its surface morphology, transmission electron microscopy was executed whereas, atomic force microscopy was carried out which contributes in detail and depth information of surface morphology. For the analysis of thermal behavior Thermal gravimetric analysis graph was obtained for luliconazole, soyalecithin, neem extract, physical mixture and optimized formulation (LF5). Attenuated total internal reflection Fourier transforms infra-red spectroscopy was performed for luliconazole, soyalecithin, neem extract, physical mixture, and optimized formulation (LF5) to examine the interaction between the drug and the excipients. Viscosity, pH, spreadability and extrudability of the ethosomal gel were calculated to determine the suitability of the formulation for topical application. In vitro drug permeation study and antifungal activity was executed out with the aid of Wistar albino rat skin model and tube dilution assay respectively. The complete study wrap up, that this herbal ethosomal approach provides advanced sustained and targeted delivery of luliconazole. On analyzing the results, ethosomal formulation LF5 was found to be optimized one, due to its optimum concentration of soyalecithin (300mg) and ethanol (35%). Hence it has maximum entrapment efficiency of 86.56 ± 0.74%. Optimum vesicle size, zeta potential, and PDI were found to be 155.30 ± 1.2nm, -42.20 ± 0.3mV, and 0.186 ± 0.07 respectively. In vitro drug permeation study expresses release of 83.45 ± 2.51 in 24h whereas; the in vivo activity proved that LF5 is more active and effective against Candida parapsilosis in comparison to Aspergillus niger. In the end, it was estimated that ethosomal suspension and lyophilized ethosomal suspension was utmost stable at 4°C/60 ± 5 RH. The complete study clearly indicates that the buildup of ethosomal formulation with luliconazole and neem extract show synergistic effect thereby, expressing excellent result against the treatment of fungal infection.

Treatment of Basal Cell Carcinoma Via Binary Ethosomes of Vismodegib: In Vitro and In Vivo Studies.

Vismodegib (VMD) is a hedgehog inhibitor which indicated for basal cell skin cancer (BCC). This work focuses on investigating the influence of isopropyl alcohol additive for topical delivering and targeting of VMD-loaded binary ethosomes for BCC treatment. Different binary ethosome formulae were prepared based on Box-Behnken design using different concentrations of phospholipid (A), cholesterol (B) and isopropyl alcohol/total alcohol ratio (C). The prepared formulae were characterized for %entrapment efficiency (R1), vesicle size (R2), %release (R3) and steady-state flux (R4). Increasing A, B and C resulted in significant increase of R1 and R2 and significant decrease of R3 and R4. The optimization was achieved and the optimum formula was selected to investigate its anti-tumour efficacy in vivo. The optimum formula showed a localized VMD and consequently a significant anti-tumour activity compared with oral VMD. Briefly, VMD-loaded binary ethosome gel could be an effective treatment of BCC with lower side effects. Graphical abstract.

Corn Silk Based Ethosomal Gel: A New Treatment for Periodontitis in Diabetic Albino Rats a Prelimenary Study

Objective: Periodontitis and diabetes are related and high blood glucose level plays an important part in this correlation. Corn silk has the property of anti‑hyperglycemic and anti‑inflammation. The aim of this study was to determine the capability of corn silk based Ethosomal gel to reduce blood glucose level and degree of inflammation in alloxan induced rats. Material and Method: 15wistar male rats with initial weight of 150gram were included in this study. Alloxan was used to induce diabetes and 5‑0 silk ligatures to induce periodontitis. Blood glucose level was analyzed before and after induction, 3 days after administration, and 7 days after. Degree of inflammation was examined with histopathology test. Results: Blood glucose level in F1 is unstable (p=0.0583>p=0.05), whilst F2 and F3 both showed stable blood glucose decrease (F2: p=0.0086<p=0.05; F3: p=0.035<p=0.05). Anti‑inflammation effects best shown in F3, which has mild inflammation (p=0.001<p=0.05).Whereas both F1 and F2 have moderate inflammation (F1: p=0.225>p=0.05; F2: p=0.423>p=0.05). Conclusion: Corn silk based Ethosomal gel treatment manage to reduce blood glucose level and periodontitis in alloxan induced diabetic rats.

Formulation and Characterization of Nanosized Ethosomal Formulations of Antigout Model Drug (Febuxostat) Prepared by Cold Method: In Vitro/Ex Vivo and In Vivo Assessment.

Febuxostat (FXT) is a xanthine oxidase (XO) drug which indicated for the treatment of gout. FXT loaded nanosized ethosomes were prepared using cold method with varied concentrations of ethyl alcohol and soya lecithin (SL). The prepared ethosomes were characterized by size, entrapment efficiency (DEE), FT-IR, in vitro release, kinetic studies of in vitro release profile, in vitro skin permeation and deposition, and stability study. The selected ethosomal formulation was incorporated in HPMC gel and characterized for drug content, ex vivo diffusion study through rat skin, and in vivo study and determination of pharmacokinetic parameters using HPLC technique. The results of size analysis showed that minimum size was 124.2 ± 16.77 nm with PDI values between 0.2 and 0.6. The zeta potential was from - 43.5 ± 3.0 to - 20.6 ± 1.42 mV. DEE ranged from 48 to 86%. The results of in vitro skin permeation showed that the amount FXT permeated ranged from 43.33 ± 5.3 to 82.14 ± 5.8%, flux ranged from 14.85 to 28.02. The results of ex vivo study showed that the amount of FXT permeated from unprocessed FXT gel was 49.42 ± 3.29% which was lesser than from FXT ethosomal gel. The results of in vivo study showed that Cmax and tmax were significantly different and higher for transdermal administration of FXT than oral administration. The developed FXT nanosized selected ethosome-based transdermal drug delivery gel system would provide a promising method for better management of gout.

Formulation and evaluation of the topical ethosomal gel of melatonin to prevent UV radiation.

Clinically, melatonin (MLT) has variable oral absorption and extensive first-pass effect, making its oral mode less preferable. Ethosomes are able to permeate intact through the human skin due to its high deformability. Present study assessed topical potential of ethosomes loaded with MLT for the prevention of UV radiation. Melatonin was encapsulated using different ratios of ethanol, soya lecithin, and cholesterol. Prepared ethosomes were characterized for scanning electron microscopy (SEM), zeta potential, % entrapment efficiency (%EE), in vitro drug release kinetics. Then, optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, in vitro skin permeation study, flux, and stability. Ethosomes were spherical in structure as confirmed by SEM, and zeta potential was in range of -12.4mV to -27.4mV. %EE of the vesicles was in the range of 49.61%-78.047%. Cumulative percentage drug release from various ethosomal formulations was ranged from 64.82%-81.01%. F3 was selected as optimized formulation on the basis of highest %EE, zeta potential, and in vitro drug release. An ethosomal gel of optimized formulation F3 was prepared by using carbopol 934 and compared with plain gel formulation. G3 formulation showed pseudoplastic rheological behavior, optimum pH, spreadability and also showed maximum % in vitro drug permeation with flux 13.85μg/cm2 /hr and followed zero-order release kinetics which was good for topical drug delivery system. This research suggested that MLT loaded ethosomes can be potentially used as a topically drug delivery system.

Thymoquinone-loaded lipid vesicles: a promising nanomedicine for psoriasis

BackgroundPsoriasis, a recurrent, chronic inflammatory disorder of skin, is a common problem in middle age and elderly people. Thymoquinone (TQ), a lipid soluble benzoquinone is the major active ingredient of volatile oil of Nigella sativa (NS), possesses good anti-psoriatic activity. However, its hydrophobicity, poor aqueous solubility, and photosensitive nature obstructs its development. Therefore, in the present research work, ethosomal vesicles (EVs) loaded with TQ were assessed for its anti-psoriatic potential employing mouse-tail model.MethodsTQ-loaded EVs were prepared by cold method, and characterized for various essential attributes, viz. particle size, morphology, percent drug entrapment, flexibility, rheological and textural analysis, and skin absorption. The optimized formulation was finally evaluated for anti-psoriatic activity on Swiss albino mice employing mouse-tail model for psoriasis.ResultsThe spherical shaped vesicles were in the nanosize range, and had high flexibility. The EVs incorporated hydrogel was rheologically acceptable and resulted in substantial TQ retention in the skin layers. The % anti-psoriatic drug activity was observed to be substantially better in the case of TQ-loaded ethosomal gel vis-à-vis plain TQ, NS extract, and marketed formulation.ConclusionsThe promising outcomes of the current studies ratify the superiority of TQ-loaded phospholipid-based vesicular systems for the management of psoriasis over other studied test formulations. This study, thus open promising avenues for topical application of TQ in the form of EV hydrogel.

Ethosomal Gel for Improving Transdermal Delivery of Thymosin β-4.

PurposeThymosin β-4(Tβ-4) is a macromolecular protein drug with potential for drug development in wound repair but is limited by the shortcomings of macromolecular protein, such as large volumes, poor membrane permeability, and unstable physicochemical characteristics. Ethosomes could enhance cell membrane fluidity and reduce epidermal membrane density to make macromolecular drugs through the stratum corneum into the deeper layers of the skin easily. Herein, we developed and characterized a novel transdermal delivery vehicle to load macromolecular protein peptides and use Tβ-4 as a model drug wrapped into ethosomes.MethodsWe used the orthogonal method to optimize the formulation of the ethosome preparation prepared by the ethonal infusion method. Ethosomal gels were characterized by using different analytical methods. Transdermal release rate in vitro have been demonstrated in Franz diffusion cells and the efficacy of drug-loaded nanocarriers in vivo was investigated in a mouse model.ResultsOptimized Tβ-4 ethosomal gels have good physicochemical properties. The drug amounts of the cumulative release in the ethosomal gel within 5 hours were 1.67 times that of the T-β4 gel in vitro release study, and the wound healing time of ethosomal gel group was only half of the T-β4 gel group in vivo pharmacokinetic study. Compared with the free drug group, the ethosome preparation not only promotes the percutaneous absorption process of the macromolecular protein drugs but also shortened wound recovery time.ConclusionHence, we provide a possible good design for ethosomal gel system that can load macromolecular protein peptide drugs to achieve transdermal drug administration, promoting the percutaneous absorption of the drug and improving the effect.

Development of Topical Gel of Methotrexate Incorporated Ethosomes and Salicylic Acid for the Treatment of Psoriasis.

There is an unmet need for optimized drug delivery system of psoriasis therapy because of various issues like adverse reaction, permeation problem associated with convention treatment (oral and topical) available for psoriasis. The goal was to develop an ethosomal gel of methotrexate (MTX)-incorporated ethosomes and salicylic acid (SA) and to evaluate and study its ethosomal gel potential in Imiquimod-induced psoriasis animal model to treat symptoms of psoriasis. MTX-SA ethosomal gel was prepared by the cold method given by Touitou et al. and optimized by comparing it with MTX ethosomal gel and drug solution. Particle size, zeta potential, entrapment efficiency, and ex-vivo study were selected as the critical quality checking attributes. Psoriatic Area and Severity Index (PASI) score & histopathological examination were done for checking Antipsoriatic potential of MTX-SA ethosomal gel by using the imiquimod-induced psoriasis model. Optimized MTX-SA exhibited a particle size of 376.04 ± 3.47nm, EE(Entrapment efficiency) of 91.77 ± 0.02%. At the end of 24h, MTX-SA ethosomal gel exhibited a slow and prolonged release of MTX (26.13 ± 1.61% versus 6.97 ± 0.06%) compared to MTX drug solution. It also attributes of 43% retention study as compared to drug solution (13%). Besides, it essentially decreased the PASI score with the recuperation of normalcy of the mice's skin, while the MTX-SA gel displayed indications of gentle hyper and parakeratosis toward the completion of investigation when contrasted with the blank gel. The developed MTX-SA ethosomal gel formulation can be a promising alternative to existing MTX formulation in topically treating psoriasis.

Gel edasi: Ethosomal gel using cow’s blood as a supportive of healing diabetic foot ulcer

Diabetes mellitus (DM) is a chronic carbohydrate metabolic disorder. Diabetic foot injury is one of the chronic complications of people with diabetes mellitus because it can cause disability and even cause death. Cow blood waste is a waste that can disturb the environment. Components of the chemical elements contained in cow blood include nitrogen, phosphorus, potassium, organic carbon, erythrocytes and leukocytes which function in the body’s defense by fighting infections so that cow blood waste is one alternative solution in the treatment of diabetic feet at a price affordable. Ethosome gel is a gel preparation that has the advantage of penetrating into the skin layer faster and significantly increasing the value of transdermal preparation flux. Based on the results of the study, the desired platelets from cow blood were obtained after sampling from the Makassar city slaughterhouse. The platelets obtained were then weighed as much as 0.5 g, 1 g, and 1.5 g to make a gel formula with a carbopol base of 1%. The gel that has been made is then evaluated like a homogeneous and clear gel physical examination. The pH obtained in formulas 1, 2 and 3 is 6.43; 7.00; and 6.80. The formula 1 has a viscosity of 47,342.6 cps and the formula 2 has a viscosity of 45,678.5 cps while formula 3 has viscosity 35,456.7 cps. In the stability test the results obtained were that the preparation did not experience changes in color and odor.

Formulation Development and Evaluation of Ethosomal Gel of Acyclovir for the Treatment of Herpes Zoster

The present study is to develop and evaluate an ethosomal gel formulation of acyclovir (ACV). It aims to provide a topical treatment for many viral infections that affect the skin. Administration of medications topically having the facility of delivering a high concentration of the drug to the skin than would be possible with systemic therapy. Topical administration of drugs is better for local action and the efficiency of the topically administered drug is increased with liposome, proliposomes and ethosomes. Recently, it was found that ethosomal carriers were phospholipid vesicular systems having relatively high concentrations of alcohol, enhances dermal and transdermal delivery of both lipophilic as well as hydrophilic molecules. ACV is the common antiviral agent that is used to treat infections caused by certain types of viruses. It treats cold sores around the mouth (caused by herpes simplex), shingles (caused by herpes zoster) and chickenpox. ACV 5% cream is used for the treatment of infection along with oral dosage forms like tablets. These formulations show poor therapeutic outcome due to the poor bioavailability (15-20%) of oral dosage forms. Ethosomes were formulated using phospholipid, ethanol, polyethylene glycol and purified water by cold method. Ethosomes were evaluated for vesicle size, shape, optical microscopy, entrapment efficiency and in-vitro release study. AEF5 have better drug entrapment efficiency than the other formulation. The best formulation (AEF5) was used to prepare gel by using carbopol 934 as a gelling agent. The ethosomes were entrapped in gel matrix of carbopol 980 in different concentration 0.5%, 1.00% and 1.5% w/w. FT-IR studies revealed no interaction between the drug and excipients. The formulated gel formulation was evaluated with parameter pH, viscosity, spreadability, in-vitro release test, washability, extrudability study and stability studies. The formulation AEG2 have better in-vitro drug release profile which contains carbopol 980 concentration 1%w/w. The present work also focuses on making the formulation more pharmaceutically acceptable. Keywords: Acyclovir, Ethosomal gel, Viral infections, Phospholipid, % Entrapment efficiency, Vesicle size

Quality by design driven development of resveratrol loaded ethosomal hydrogel for improved dermatological benefits via enhanced skin permeation and retention

Resveratrol is a potent anti-oxidant agent and can be used for the effective management of different skin conditions like extrinsic skin ageing, psoriasis, etc. The objective of this research was to develop a dermal delivery system of resveratrol for its improved dermatological benefits for achieving its enhanced skin deposition profile with limited systemic exposure. Resveratrol loaded ethosomal hydrogel was developed and optimized using systematic Quality by Design approach. Firstly, the quality target product profile (QTPP) of ethosomal formulation was defined and critical quality attributes (CQAs) and critical material attributes (CMAs) were screened through risk assessment studies based on fish bone diagram. 32 full factorial design using Design Expert software was employed to optimize the selected CMAs. Concentration of phospholipid (X1) and concentration of ethanol (X2) were selected as independent CMAs. Vesicle size (Y1), entrapment efficiency (Y2), permeation flux (Y3) and drug deposition in dermal layer (Y4) were evaluated as dependant CQAs. Optimized formulation was then evaluated for physicochemical and skin permeation properties. Ethosomal hydrogel was able to significantly enhance the skin permeation parameters and skin deposition of resveratrol in comparison to the conventional cream. The results were highly ratified by CLSM studies in which ethosomal hydrogel was found to be vastly scattered in the deeper skin layers. Thus, there is evidence that systemically developed ethosomal gel can deliver enhanced amounts of bioactives into the skin and it is expected that a number of products for dermal/transdermal applications will be developed in the future based on it.

Skin permeation enhancement of nicotinamide through using fluidization and deformability of positively charged ethosomal vesicles: A new approach for treatment of atopic eczema

For the treatment of atopic eczema, the drug penetration of the relevant skin layers is considered to be a major scientific concern. In this study, a new formulation which is based on positively charged ethosomes as drug carriers were prepared and evaluated for their efficacy in penetrating the stratum corneum and accumulating in the skin. The proposed mechanism of skin permeation and retention is based on the dual effect of ethanol as the main component of the ethosomes and stearylamine as a positive charge inducer. A statistical Box- Behnken experimental design was deployed in this study with the use of three variables at three levels; phospholipid concentration, propylene glycol concentration, and ethanol concentration. The prepared formulations were characterized for entrapment efficiency, vesicle size and percent drug released after 6 h. The vesicle size of the prepared formulations was ranging between 18.12 ± 9.19 and 528.1 ± 21.75 nm, while the entrapment efficiency ranged between 86.92 ± 1.34 to 94.15 ± 1.41% and percent drug released after 6 h was ranging between 6.73 ± 0.12 and 99 ± 3.12%. After entering the different responses of the formulations into the statistical software, two formulations were generated as optimized formulations and subjected to the study of the effect of stearylamine as a positive charge inducer on the retention of nicotinamide inside the skin. In vivo testing of the thermosensitive positively charged ethosomal gel of nicotinamide on induced eczema in animal models revealed an enormous recession of inflammatory reaction associated with eczema in addition to the significant reduction of corneocytes maturation.

SYNERGISTIC EFFECT OF NIGELLA OIL AND CLOTRIMAZOLE AS ETHOSOMAL GEL FOR IMPROVED TREATMENT OF FUNGAL INFECTIONS

The aim of this research work was to develop an ethosomal gel containing nigella oil encapsulated with clotrimazole (CLT) for improved antifungal activity. The ethosomes were prepared using soya lecithin (SpC) and Nigella oil (NO) as lipids by thin film hydration and they exhibited a particle size of 136±69 nm with an entrapment efficiency of 65.44±1.08 %. CLT ethosomal gel exhibited controlled release of CLT with a steady flux of 7.20mcg/cm2/h across cellophane membrane. The ethosomal gel was stable for 180 days with no significant change in physiochemical parameters. In vitro antifungal activity demonstrated a synergistic action of CLT and NO against the fungal strains compared to plain CLT and NO. This signifies that the combination of NO and CLT in an ethosomal gel has tremendous potential to serve as a synergistic topical anti-fungal preparation than simple ethosomal formulation of CLT.

Design by optimization and comparative evaluation of vesicular gels of etodolac for transdermal delivery

Aim of the present study was to design vesicular gels of etodolac loaded liposomes and ethosomes for effective transdermal delivery. The physicochemical properties of vesicular gels were compared with 45% v/v ethanolic etodolac solution and commercial product (PROXYM®). The liposomes were prepared by film hydration technique whereas ethosomes were prepared by cold method respectively. Both the systems were characterized for various physicochemical properties. The size range of liposomes shows 186 nm–363 nm whereas for ethosomes 170 nm–261 nm respectively. The zeta potential of optimized liposomes and ethosomes was found to be −36.5 mV and −48.3 mV, respectively. The highest %EE of liposomes and ethosomes shows 71.5% and 78.5%, respectively. The permeation of liposomes shows in the range of 67.50%–86.06% whereas ethosomes shows 52.30%–99.49%, respectively. The optimization was done by 32 experimental design. The optimized vesicular dispersions were subjected to gel preparation using carbopol 940 NF. The prepared liposomal gel (ETO-LG) and ethosomal gel (ETO-EG) were optimized and characterized. The vesicular gels showed desirable results compared to other test formulations.

Curcumin Loaded Ethosomal Vesicular Drug Delivery System for the Treatment of Melanoma Skin Cancer

Curcumin has an excellent safety profile having various pleiotropic actions, including anti-inflammatory, antioxidant, antitumoral, anticancer, and antimicrobial activities, with the potential for neuroprotective activity but the poor oral bioavailability limits its use as oral dosage form. The purpose of this study was to formulate and evaluate the transdermal drug delivery system of Ethosomes containing curcumin, a potent anti-cancer drug. Study on various formulation excipients revealed that all the excipients shown some variation which affected the vesicle size, zeta potential, PDI and entrapment efficiency. Batch prepared with 10 % of soya lecithin, 4.5 % of ethanol and 10% of cholesterol showed maximum entrapment efficiency of 81.2±3.12.In in vitro drug permeation studies using dialysis bag, the samples withdrawn in equal time intervals shown more drug release from the dialysis bag in comparison with that of inhouse paclitaxel gel which conform that the curcumin loaded ethosomal gel is a better formulation for the further studies. In ex vivo, permeation study using pork ear skin, curcumin loaded ethosomal gel showed the greater drug deposition on the skin > 60 % in 12 hrs for the better curability for the melanoma. Whereas inhouse paclitaxel gel shown < 60 % of drug deposition in 12 h. The comparison of both ethosomal gel and inhouse paclitaxel gel reveals that ethosomal gel shown maximum release within 12 hrs in both in vitro and ex vivo studies, which can be taken for the further in vitro cell line and in vivo study.

DEVELOPMENT OF TERMINALIA CHEBULA LOADED ETHOSOMAL GEL FOR TRANSDERMAL DRUG DELIVERY

Objective: Oral route is the usual route of drug delivery which has many advantages such as easy delivery but has disadvantages such as poor bioavailability and tendency to produce rapid blood level spikes, such that there becomes a necessity for higher dose or recurrent dosing which becomes difficult for the patient and also high cost. Keeping all these drawbacks in concern, there arises a necessity for novel development of drug delivery with improved therapeutic efficacy and safety with targeted delivery such that size and number of doses could be reduced. This can be achieved by transdermal delivery which possesses several advantages such as avoids first-pass metabolism, eliminates gastrointestinal irritation reduces frequency of dosing, and rapid termination of drug action.Methods: Dried fruits of Terminalia chebula were extracted and preliminary phytochemical evaluation was performed. Ethosome was prepared by cold method using soya lecithin. Ethosomal gel was prepared using carbopol as gelling agent and was evaluated.Results and Discussion: The prepared gel was evaluated for its pharmaceutical properties and was found to be satisfactory. The in vitro drug diffusion of ethosomal gel showed better release compared with that of the gel with extract. In vitro anti-arthritic activity exhibited significant effect compared to that of the standard diclofenac.Conclusion: Considering all the above-mentioned factors, the present study was aimed to develop a natural drug-loaded ethosomal gel for transdermal drug delivery, thereby permeation of drug can be enhanced compared with conventional dosage forms.