Transferosomal Gel Research Articles

Formulation and evaluation of Lamivudine transferosomal gel

Aim and objective: The aim of the study was to formulate and evaluate Transferosomal gel of lamivudine.
 Method:Lamivudine transferosomes was prepared using thin film hydration method taking span 80, Polyoxyethylene lauryl ether in different proportion. the formulation was characterised by UV spectroscopy, FTIR, in-vitro drug release, gel evaluations.
 Results: Total nine formulations were formulated and optimised formulation F3 showed entrapment efficiency EE (91.17), %CDR (96.12) and small particle size (98.19 nm). SEM of optimized lamivudine Transferosomes appeared as spherical, well identified, unilamellar vesicles. The optimized formulation of Transferosomes was further formulated to gel with Poloxamer 407 gel 0.5%, 1% and 2% w/w ,HPMC k15, Propylene glycol, DMSO. Among these F3 formulation with Poloxamer 407 2%w/w transferosomal gel is the optimised transferosmal gel and showed Spreadability value 6.01±0.12 cm, pH value 5.01 ±0.47. The actual drug content of the Transferosomal gel was found to be 97.29 ±0.66%, which represents good content uniformity. The viscosity of lamivudine Transferosomal gel is found to 5960 ±0.75cps. The percentage drug release for lamivudine Transferosomal gel is 97.31 %. stability studies showed that Transferosomal gel is more stable at 4˚C when compared to other temperatures. The future scope of the study is to perform the In Vivo studies to evaluate the potency of the prepared formulation.
 Keywords: Lamivudine Transferosomal gel, Transferosomes, Topical, Anti-viral drug, Thin Film Hydration Technique.

Formulation and evaluation of Lamivudine transferosomal gel

Aim and objective: The aim of the study was to formulate and evaluate Transferosomal gel of lamivudine.
 Method:Lamivudine transferosomes was prepared using thin film hydration method taking span 80, Polyoxyethylene lauryl ether in different proportion. the formulation was characterised by UV spectroscopy, FTIR, in-vitro drug release, gel evaluations.
 Results: Total nine formulations were formulated and optimised formulation F3 showed entrapment efficiency EE (91.17), %CDR (96.12) and small particle size (98.19 nm). SEM of optimized lamivudine Transferosomes appeared as spherical, well identified, unilamellar vesicles. The optimized formulation of Transferosomes was further formulated to gel with Poloxamer 407 gel 0.5%, 1% and 2% w/w ,HPMC k15, Propylene glycol, DMSO. Among these F3 formulation with Poloxamer 407 2%w/w transferosomal gel is the optimised transferosmal gel and showed Spreadability value 6.01±0.12 cm, pH value 5.01 ±0.47. The actual drug content of the Transferosomal gel was found to be 97.29 ±0.66%, which represents good content uniformity. The viscosity of lamivudine Transferosomal gel is found to 5960 ±0.75cps. The percentage drug release for lamivudine Transferosomal gel is 97.31 %. stability studies showed that Transferosomal gel is more stable at 4˚C when compared to other temperatures. The future scope of the study is to perform the In Vivo studies to evaluate the potency of the prepared formulation.
 Keywords: Lamivudine Transferosomal gel, Transferosomes, Topical, Anti-viral drug, Thin Film Hydration Technique.

Formulation and Ex vivo Permeation Study of Tamoxifen Citrate Loaded Transfersomal Gel

Objective: The current study’s objective is to assess the transfersomal gel, administration of tamoxifen citrate transdermally for DEPARTMENT OF Expenditure (DOE) Approach. Materials and Methods: Supramolecular clusters with extreme flexibility, known as transferosomes can penetrate untouched animal skin. The formulations were designed by Box-Behnken design (BBD). The ex-vivo skin permeation study of tamoxifen citrate-loaded transferosomal gel was compared with commercial gel and blank drug solution. A total of 100 mg of the maximal drug release (94.32%) from the tamoxifen citrate optimized transferosome formulation demonstrated excellent results. Conclusion: According to this study, the comparatively stable transferosomes represent a promising long-term administration strategy for tamoxifen citrate. According to this study, transdermal drug delivery of skin cancer could be treated by employing transferosomes containing the tamoxifen citrate.

Box-Behnken Design: Optimization of Proanthocyanidin-Loaded Transferosomes as an Effective Therapeutic Approach for Osteoarthritis.

Transferosomes are one of the vesicular carriers that have received extensive research and attention recently because of their capacity to get beyond the barriers posed by the stratum corneum to penetration. The intent of the current study is to optimize and evaluate proanthocyanidin (PAC) containing transferosomal transdermal gels. PAC-containing transferosomes were prepared using the film hydration method and then loaded into a 4% methylcellulose gel. A 23 Box–Behnken design was used to optimize the PAC-loaded transferosomal gel, where the effects of phospholipid 90 G (X1), Tween 80 (X2), and sonication time (X3) were evaluated. The formulation factors, such as the drug entrapment efficiency percentage (PEE) and in vitro drug release, were characterized. A PEE of 78.29 ± 1.43% and a drug release in vitro at 6 h of 24.2 ± 1.25% were obtained. The optimized transferosomal-loaded proanthocyanidin (OTP) formulation penetrated the porcine skin at an excellent rate (0.123 ± 0.0067 mg/cm2/h). Stability tests were conducted for OTP to predict the effects of various temperature conditions on the physical appearance, drug content, and PEE for periods of 15, 30, and 45 days. Finally, this transferosomal system for transdermal PAC delivery may be a suitable alternative to the conventional treatment for osteoarthritis.

Design and development of tofacitinib citrate loaded transferosomal gel for skin cancer by box-Behnken design- doe approach

Objective: The purpose of the present study is to develop, statistically optimize and evaluate the transfersomal gel formulation of Tofacitinib citrate via transdermal route by DOE Approach. Materials and Methods: Transferosomes are made up of with bilayer forming phospholipids and biocompatible surfactants like sodium deoxycholate. The surfactants also acts as edge activator which stabilizes the phospholipid bilayer and increases the deformability of the vesicle. The formulation were designed by Box-Behnken Design. For usage as a transferosomal gel, drug encapsulation in various transfersomal formulations having 100 mg drug concentrations and Carbopol-934 (0.5,1.2 g) is being studied. Results: Entrapment efficiency (EE percent), drug content, in-vitro skin penetration testing, and stability studies were all found in the produced formulations. Transmission Electron Microscopy confirmed that the vesicles were spherical in shape. According to the findings, Tofacitinib citrate was effectively pinned with a standardised drug concentration in all formulations. The 0.1 g Tofacitinib citrate optimised transferosome formulation TG2 exhibited encouraging results, with maximum drug release (94.32%). Conclusion: Transferosomes are a promising long-term delivery route for Tofacitinib citrate and are relatively stable. This research work reveals that transferosomes containing Tofacitinib citrate could be used to treat squamous cell carcinoma via transdermal drug delivery.

Formulation and in-vitro evaluation of Bosewellia Serrata extract loaded transferosomal gel for treatment of osteoarthritis

Objective: The main objective of the current research work was to formulate and evaluate Bosewellia serrata extract loaded transferosomal topical gels. To overcome the drawbacks associated with oral administration of Bosewellia serrata extract in Osteoarthritis treatment. Methodology: Transferosomes were developed using different ratios of Phospholipon® 90G as phospholipid, Span-60 as surfactant and cholesterol as fluidity buffer. The selected best formulation of transferosomes was further optimized as a topical gel using different rate controlling polymers such as hydroxylethyl cellulose (HEC), hydroxyl propyl methylcellulose (HPMC) and, carbopol. Transcutol P was used as a penetration enhancer. In vitro diffusion studies of developed formulations were carried out using Franz diffusion cell apparatus. Results: Formulation BT10 prepared with 2:1 ratio of drug to total lipid, 2:1 ratio of surfactant to total lipid and 3:1 ratio of phospholipid to cholesterol was selected as optimized transferosomes. Further transferosomal gel was formulated by trial and error method, where different polymers considered as gelling agents. Transcutol HP and glycerol used as penetration enhancer and bodying agent respectively. Among the twelve formulations, BG11 (Carbopol 971 in 0.75% w/w) was chosen as the best formulation due to controlled invitro release of the drug with very good viscosity and spreadabilty.

Formulation and in vitro Evaluation of Diacerein Loaded Transferosomal Topical Gel for the Effective Treatment of Osteoarthritis

Aim: The main objective of the current research work was to formulate and evaluate Diacerein-loaded transferosomal topical gel to overcome the drawbacks associated with oral administration of Diacerein in Osteo arthritis treatment.
 Study Design: Transferosomal topical gel
 Methodology: Transferosomes were developed using different ratios of Phospholipid® 90G as phospholipid and Span-60 as surfactant and cholesterol as fluidity buffer. The selected best formulation of transferosomes was further optimized as a topical gel using different rate controlling polymers such as hydroxylethyl cellulose (HEC), hydroxyl propyl methylcellulose (HPMC) and, carbopol. Transcutol P was used as a penetration enhancer. In vitro diffusion studies of developed formulations were carried out using Franz diffusion cell apparatus.
 Results: The formulations prepared with Hydroxy ethyl cellulose (TBG1, TBG2, TBG3), HPMC (TBG4, TBG5, TBG6) was shown rapid drug release when compared to formulations prepared with carbopol (TBG7, TBG8, TBG9) are showing controlled drug release.Where the formulation prepared with carbopol with 0.75% concentration has shown acceptable extended drug release for 12 hours with acceptable other physico-chemical properties.
 Conclusion: It can be concluded that Diacerein-loaded transferosomal gel can be administered topically for the treatment of osteoarthritis with reduced oral side effects.

Formulation, Evaluation, and Optimization of Diacerein Loaded Transferosomal Gel for Arthritis

The objective of the current study was to develop and evaluate diacerein-loaded transferosomal gel to augment the permeation of diacerein into the deeper skin layer and finally to the affected area to treat arthritis. Preliminary studies included the process variable optimization (RPM) and selection of surfactant. The circumscribed central composite design was included to explore the reactions of the amount of phospholipon 90H, cholesterol, and span 60 on dependent variables like % entrapment co

Formulation and evaluation of fusidic acid based transferosome for burn wound infection

Transferosome, being very flexible and deformable nature to cross stratum corneum are selected for enhancing the transdermal delivery of fusidic acid. The present research work comprised formulation of fusidic acid transferosome using modified reverse phase evaporation process and characterised for particle size, zeta potential, entrapment efficiency and in vitro drug release. An optimised formulation of transferosome made by Phosphatidyl choline S100 and Span 80 (F2) showed lowest size of 145.16 nm and high drug entrapment efficiency of 87.47 ± 0.119. 2 %w/v Carbopol based transferosomal gel formulation (N4) of Fusidic acid showed entrapment efficiency 78.22% and Fickian diffusion-based release mechanism with 47% and 94% drug release at 6 h and 24 h respectively. The promising results from the current study can be exploited in future research for in-vivo performance.

Formulation Development and Evaluation of Transfero-somes Nano Gel Loaded with Levocetirizine Transfero-somes

A new drug delivery technology called transferosomes were came into existence which is an artificial vesicle designed to show the characteristics of a cell vesicle suitable for controlled and potentially directed drug delivery. Transferosome is a highly flexible and stress- responsive compound, complex compound and highly deformed vesicle with an aqueous core surrounded by the complex lipid bilayer thus enabling it to deliver both hydrophilic and hydrophobic drug. Urticaria is a general condition distinguished as brief erythematous and oedematous plaques or papules with defined erythematous borders and central clearing, identified as hives/wheals. Levocetirizine which is used for the treatment is a H1 anti histamine that is actively used in treatment of urticaria. The aim of the present research work was to investigate the potential of transferosome formulations for transdermal delivery of levocetirizine. The transferosomes were formulated by lipid film hydration technique using Rotary vacuum Evaporator. In the present work levocetirizine vesicle was efficaciously formulated using an appropriate ratio of tween 80 and soya lecithin and was incorporated into gel since gel formulations are easy to administer and patient compliance. Levocetirizine transferosomes was evaluated for vesicle characteristicslike zeta potential, poly-dispersibility index, TEM, and stability study. Theaverage sizes of transferosome were found to be 566.6nm and poly dispersity index (PI) was found to be 0.532, zeta potential of the transferosome was found to be -2.3 mV which indicates that transferosome formulation is stable. Levocetirizine gel was prepared by using various concentrations of Carbopol 934 and is evaluated for their gel characteristics like pH, viscosity, Spreadability, extrudability, homogeneity, drug content, diffusion etc. Gel containing 2% Carbopol show best and promising results. Levocetirizine transferosomal gel were efficaciously formulated by utilizing levocetirizine transferosome which was prepared by thin film hydration method by using soya lecithin and tween 80 in the ratio 85:15. Other Oral formulation used in treatment for urticaria have disadvantage like poor bioavailability, 1st pass metabolism, patient non-compliance etc. Transferosome nano gel loaded with levocetirizine transferosome was found to be more effective than other oral formulations used in treatment for urticaria since transferosome are capable of passing through lipid layer and delivering drug into systemic circulation with maximum bioavailability.

Allopurinol Loaded Transferosomes for the Alleviation of Symptomatic After-effects of Gout: An Account of Pharmaceutical Implications

Background: The present study assessed the transdermal potential of transferosomes loaded with allopurinol for the treatment of gout. Methods: Transferosomes of allopurinol were composed of different ratios of tween-80, soya lecithin and solvent using a thin-film hydration method. Transferosomes were characterized for Scanning Electron Microscopy (SEM), zeta potential, % entrapment efficiency (%EE), Fourier Transform Infrared Spectroscopy (FTIR), in-vitro drug release and kinetics as well as stability. Then, optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, ex vivo skin permeation study, flux, and stability. Results: SEM studies suggested that vesicles were spherical and zeta potential were in the range of -11.4 mV to -29.6 mV and %EE was 52.4- 83.87%. FTIR study revealed that there was no interaction between allopurinol and excipients during the preparation of transferosomes. The cumulative percentage of drug release from various transferosomes was ranged from 51.87 to 81.87%. A transferosomal gel of F8 formulation was prepared using dispersion method reported pseudoplastic rheological behavior, optimum pH, spreadability and maximum drug permeation i.e. 79.84% with flux 13.06 g/cm2/hr, followed zero-order release kinetics. Irritation and in-vivo studies of optimized transferosomal gel G8 on rabbits revealed better results than the standard allopurinol. Conclusion: This research suggested that allopurinol loaded transferosomal gel can be potentially used as a transdermal drug delivery system for the treatment of gout.

Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

Transferosomes as nanocarriers for drugs across the skin: Quality by design from lab to industrial scale.

Transferosomes, also known as transfersomes, are ultradeformable vesicles for transdermal applications consisting of a lipid bilayer with phospholipids and an edge activator and an ethanol/aqueous core. Depending on the lipophilicity of the active substance, it can be encapsulated within the core or amongst the lipid bilayer. Compared to liposomes, transferosomes are able to reach intact deeper regions of the skin after topical administration delivering higher concentrations of active substances making them a successful drug delivery carrier for transdermal applications. Most transferosomes contain phosphatidylcholine (C18) as it is the most abundant lipid component of the cell membrane, and hence, it is highly tolerated for the skin, decreasing the risk of undesirable effects, such as hypersensitive reactions. The most common edge activators are surfactants such as sodium deoxycholate, Tween® 80 and Span® 80. Their chain length is optimal for intercalation within the C18 phospholipid bilayer. A wide variety of drugs has been successfully encapsulated within transferosomes such as phytocompounds like sinomenine or apigenin for rheumatoid arthritis and leukaemia respectively, small hydrophobic drugs but also macromolecules like insulin. The main factors to develop optimal transferosomal formulations (with high drug loading and nanometric size) are the optimal ratio between the main components as well as the critical process parameters for their manufacture. Application of quality by design (QbD), specifically design of experiments (DoE), is crucial to understand the interplay among all these factors not only during the preparation at lab scale but also in the scale-up process. Clinical trials of a licensed topical ketoprofen transferosomal gel have shown promising results in the alleviation of symptons in orthreothritis with non-severe skin and subcutaneous tissue disorders. However, the product was withdrawn from the market which probably was related to the higher cost of the medicine linked to the expensive manufacturing process required in the production of transferosomes compared to other conventional gel formulations. This example brings out the need for a careful formulation design to exploit the best properties of this drug delivery system as well as the development of manufacturing processes easily scalable at industrial level.

Formulation, Development and Evaluation of Transfersomal Gel of Metronidazole

Metronidazole is an antibiotic that is used to treat a wide variety of infections. It works by stopping the growth of certain bacteria and parasites. This antibiotic treats only certain bacterial and parasitic infections. It may also be used with other medications to treat certain stomach/intestinal ulcers caused by bacteria (H. pylori). A transferosome is the first generation of an elastic liposome prepared from phospholipids and edge activators. An edge activator is often a single-chain surfactant with a high radius of curvature that destabilizes the lipid bilayers of vesicles and increases the deformability of the bilayers, thereby making the vehicle ultra-deformable. The aim of the present study was to investigate the potential of transfersomal gel formulations for transdermal delivery of metronidazole and to evaluate the effect of lipid concentration, ethanol concentration, drug concentration and stirrer time. Characterization of transfersomes performed by vesicle size, surface charge, entrapment efficiency and zeta potential. Characterization of transfersome containing gel performed by the measurement of viscosity, drug content, extrudability study, spreadability and in vitro drug diffusion study. It was found that viscosity of prepared gel was 3560cps, % assay was 98.89±0.45, extrudability was 1156g and spreadibility (g.cm/sec) was found that 11.23(g.cm/sec) respectively. In vitro drug release from transfersomes gel was carried out using Franz diffusion cell method and found 85.56% in 12 hr. In first 30 min it was 22.2 % drug release which slightly high. It was due to the release of free drug present in bag after leaching from transfersomes. Drug release from transferosomal gel formulation was found in very sustained and controlled manner. The results were obtained which showed that transfersomal gel was a promising candidate for transdermal delivery with targeted and prolonged release of a drug. It also enhances skin permeation of many drugs. Keywords: Transfersomal gel, Metronidazole, Antibiotic, Characterization, Franz diffusion cell

Design, Optimization and Characterization of a Transferosomal Gel of Acyclovir for Effective Treatment of Herpes Zoster

A transferosome is the first generation of an elastic liposome prepared from phospholipids and edge activators. An edge activator is often a single-chain surfactant with a high radius of curvature that destabilizes the lipid bilayers of vesicles and increases the deformability of the bilayers, thereby making the vehicle ultra-deformable. Acyclovir is a synthetic purine nucleoside analog derived from guanine, is the most widely used antiviral agent. It is effective in the treatment of herpes simplex virus (HSV), mainly HSV-1 and HSV-2 and varicella-zoster virus. However, it has low skin permeability. Hence, the objective of this study was to prepare acyclovir using transferosomes to overcome the barrier function of the skin. The present study deals with the development of transferosomal gel containing acyclovir by handshaking method for painless acyclovir delivery for use in the treatment of skin disease through 33 Fractional factorial design in which amount of Phospholipid (A), Cholesterol (B) and Tween 80 (C) was selected as independent variables and vesicle size (X1) Polydispersity index (X2) and %entrapment efficiency (X3) as dependent variables. The prepared transferosomes were evaluated with respect to entrapment efficiency (EE %), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of acyclovir transferosomes was incorporated into a Carbapol 934 gel base which was evaluated for drug content, pH, spreadability, viscosity and in vitro permeation. The prepared acyclovir transferosomes had a high EE% ranging from 65 to 81%, with small particle sizes ranging from 181.9 to 401.8nm. The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. The formulation TF2 have better in-vitro drug release profile which contains carbopol 980 concentration 2 %w/w. The kinetic analysis of release profiles of TF2 was found to follow the Korsmeyer-Peppas model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). Therefore, acyclovir in the form of transferosomes can penetrate the skin, overcoming the stratum corneum barrier.

Nanosized Transferosome-Based Intranasal In Situ Gel for Brain Targeting of Resveratrol: Formulation, Optimization, In Vitro Evaluation, and In Vivo Pharmacokinetic Study.

Resveratrol (RES) is a potent antioxidant used for the management of several central nervous system diseases. RES bioavailability is less than 1 owing to its low solubility and extensive intestinal and hepatic metabolism. The aim of the study was to enhance RES bioavailability through developing intranasal transferosomal mucoadhesive gel. Reverse evaporation-vortexing sonication method was employed to prepare RES-loaded transferosomes. Transferosomes were developed via 34 definitive screening design, using soya lecithin, permeation enhancers, and surfactants. The optimized formula displayed spherical shape with vesicle size of 83.79 ± 2.54nm and entrapment efficiency (EE%) of 72.58 ± 4.51%. Mucoadhesive gels were prepared and evaluated, then optimized RES transferosomes were incorporated into the selected gel and characterized using FTIR spectroscopy, in vitro release, and ex vivo permeation study. Histopathological examination of nasal mucosa and in vivo pharmacokinetic study were conducted. In vitro drug release from transferosomal gel was 65.87 ± 2.12% and ex vivo permeation was 75.95 ± 3.19%. Histopathological study confirmed the safety of the optimized formula. The Cmax of RES in the optimized RES trans-gel was 2.15 times higher than the oral RES suspension and AUC(0-∞) increased by 22.5 times. The optimized RES trans-gel developed intranasal safety and bioavailability enhancement through passing hepatic and intestinal metabolism.

Preparation and optimization of lidocaine transferosomal gel containing permeation enhancers: a promising approach for enhancement of skin permeation.

AimTo develop the topical gel containing transferosomal lidocaine as alternative to painful local anesthetic injection.Materials and methodsThe transfersomes were prepared by film hydration technique using soybean phosphatidylcholine and cholesterol. The prepared transfersomes were evaluated for the morphology, drug loading, %EE, particle size and in vitro release. The transferosomal gel of lidocaine was prepared using HPMC k15 as gelling agent and propylene glycol, dimethyl sulfoxide (DMSO), and polyamidoamine dendrimer third generation (PAMAM G3) solutions were used as permeation enhancer. The formulated gels were evaluated for pH, viscosity, drug content and ex-vivo permeation of the gel. The analgesic effect of the formulation was tested using tail flick test.ResultsThe transfersomes showed that transfersomes (F4) had the highest entrapment efficiency (%EE) approaching 79.87±2.35, low particle size 179.5 nm, and zeta potential of −43.5±4.74 mV. According to the rat tail flick test, the AUC0–90 minutes of the control formulation (lidocaine solution, A) was 352.32±5.87 seconds minutes. While the maximum AUC0–90 minutes value was found to be 570.5±6.81 seconds minutes for gel formulation (F) containing transfersomal lidocaine with PAMAM G3 dendrimer as permeation enhancer. In this case, the local anesthetic efficacy was increased by 1.62-folds as compared to control formulation.ConclusionFrom the present study, it can be concluded that the topical gel loaded with transfersomal lidocaine shows enhanced skin permeation effect along with increase in local anesthetic action of lidocaine.

Effect of Various Surfactants in the Formulation and Evaluation of Etoricoxib Loaded Transferosomal Gel

Effect of Various Surfactants in the Formulation and Evaluation of Etoricoxib Loaded Transferosomal Gel

Sertaconazole nitrate loaded nanovesicular systems for targeting skin fungal infection: In-vitro, ex-vivo and in-vivo evaluation

The aim of this study was to develop different vesicular systems for sertaconazole nitrate and evaluate the ability of targeting deep skin layers to treat dermal fungal infection. Therefore, different phospholipid based nanovesicles, namely liposomes, glycerosomes, transferosmes and ethosomes were prepared and in-vitro evaluated for morphology, entrapment efficiency, vesicle size and zeta potential value, followed by ex-vivo evaluation through skin penetration and permeation. The selected vesicular formula was incorporated into gel base system and assessed by ex-vivo permeation visualization study using confocal laser scanning microscopy (CLSM). In-vivo study was performed to compare antifungal efficacy of STZL loaded vesicular gel with commercial cream (Dermofix®). All nanovesicles were unilamller and almost spherical in shape. Entrapment efficiency, vesicle size and zeta potential were dependent upon vesicle composition. Vesicular formulae promoted drug permeation compared to commercial cream where transferosomal system containing 3% soyphospholipid (SPC) and 0.15% sodium deoxychloate (SDC) exhibited highest flux (645μg/cm2/h). The CLSM images confirmed the penetration of the developed probe-loaded tansferosomal system to viable epidermis layers with fluorescence intensity greater than unencapsulated probe. The in-vivo study revealed significant prevention effect in immunecompromised rat model. Furthermore, the antifungal activity with lowest histopathological changes was significantly observed in the developed STZL-loaded transferosomal gel compared to commercial cream using immunecompromised rat model with fungal skin infection.

Transferosomal gel for transdermal delivery of risperidone: Formulation optimization and ex vivo permeation

Among these vesicular carriers, transferosomes are widely investigated and are gaining importance recently due to their ability to overcome the permeation difficulties through the stratum corneum. The objectives of the current investigation were to optimize and evaluate transferosomal transdermal gels containing risperidone. Transferosomes containing risperidone were formulated by reverse-phase evaporation and were transferred to 4% methylcellulose gel. The lipid and surfactant ratios on drug entrapment efficiency (DEE) and ex vivo risperidone permeation flux (Jss) of transferosomal gels through skin were optimized. The optimized formulation showed 61.54 ± 2.14% DEE, 589.50 nm average vesicle diameter and – 20.90 mV zeta potential. Jss of optimized gel was measured as 0.2387 ± 0.0245 μg/cm2/h. This tranferosomal system for transdermal risperidone delivery could be a better alternative over the conventional therapy.