Transferosomal Gel Research Articles

Development and Optimization of Transferosomal Gel for Efficient Topical Delivery of Berberine Hydrochloride

Background: Berberine is an isoquinoline alkaloid with potent anti-inflammatory effects. However, its therapeutic efficacy is often restricted by its poor solubility, absorption, and permeability, especially in topical applications. Transferosomes are elastic vesicular carriers with high skin permeability values and retention, making them suitable for encapsulating hydrophilic and lipophilic actives. Objective: The objective of this research was to develop a transferosome-based topical gel formulation of Berberine hydrochloride (BER) to improve its skin permeability and anti-inflammatory efficacy. Method: The thin film hydration method was used to formulate the BER transferosomes. The effects of independent variables, amount of BER in lipid phase (X1), and lipid (Phospholipon 90G) to surfactant ratio (X2) on BER entrapment and vesicle size were studied using face-centered central composite design. The characterization was performed using differential scanning calorimetry, transmission electron microscopy, and X-ray diffraction. The optimized batch (F5) was incorporated in Carbopol gel and further investigated for viscosity, in vitro and ex-vivo diffusion, skin retention by tape stripping, and in-vivo anti-inflammatory efficiency. Results: The formulation optimized with 50 mg of drug and a 5:1 lipid-to-surfactant ratio (F5) demonstrated higher drug entrapment efficiency (72.11%) and lower vesicle size (77.9 nm). TEM validated the spherical vesicle morphology, whereas DSC and XRD analysis confirmed the molecular entrapment of BER within the phospholipid vesicles. The transferosomal gel demonstrated improved BER diffusion (0.63 mg/cm2) confirmed by in vitro and ex-vivo diffusion experiments that revealed a 6-fold increase in flux and permeability coefficient (0.1053 mg. cm-2.h-1). The drug release from transferosome gel was non-Fickian in nature (n = 0.6575), indicating an integration of diffusion and erosion processes. Furthermore, BER transferosomal gel displayed substantial anti- inflammatory activity in rats (p < 0.001). result: The independent variables exerted a substantial impact on drug entrapment and transferosome vesicle size. The optimized batch (F5) exhibited 72.11 % of BER entrapment and 77.9 nm vesicle size. DSC studies indicated molecular dispersion of BER in phospholipon G. The change in BER crystalline state was indicated by the XRD study. In vitro, diffusion study of Transferosome gel formulation indicated the sustained release by a non-fickian mechanism. Ex vivo skin permeation revealed significant improvement in BER permeation (p< 0.05). Further, the tape-stripping method revealed higher BER skin permeability. In-vivo anti-inflammatory efficacy of BER transferosome gel was significantly higher as compared to plain BER gel. Conclusion: The findings demonstrated the potential of transferosomal gel as a promising approach for efficient drug delivery and therapeutic efficacy.

Quality by design-based optimization of teriflunomide and quercetin combinational topical transferosomes for the treatment of rheumatoid arthritis

Rheumatoid arthritis (RA) is an immune-mediated inflammatory disease. Combination therapy is anticipated to surpass monotherapy by targeting multiple pathways involved in RA progression. The present aim is to develop a combination of Teriflunomide (TFD) and Quercetin (QCN) loaded transferosomal gel to enhance permeability and achieve localized delivery to joint tissues. TFD or QCN transferosomes were optimized employing a 3-level, 3-factorial design Box-Behnken design (BBD). The transferosomes exhibited sustained in-vitro drug release. The topical combination gel underwent thorough evaluation of rheology, and also ex-vivo studies showed enhanced permeability through rat skin. The synergistic combination of TFD and QCN effectively suppressed NO, TNF-α and IL-6 levels in in-vitro RAW 264.7 cells. The cytotoxicity in HaCaT cell lines indicates non-toxicity of the gel, further confirmed by skin irritation study conducted in rats. The in-vivo anti-arthritic activity was evaluated in complete freund’s adjuvant induced rat paw edema model illustrates the effectiveness of the combination transferosomal gel compared to other treatment groups. In conclusion, the topical delivery of TFD and QCN combination transferosomal gel demonstrated anti-arthritic activity through localized delivery whichallows for dose reduction, thereby may reduce the systemic drug exposure and mitigate the side effects associated with oral administration of TFD.

Formulation and Evaluation of Acyclovir Loaded Transferosomal Gel for Transdermal Drug Delivery

Background: A carrying structure for targeted transdermal drug delivery is a transferosome. These unique liposomes are made of an edge activator and phosphatidylcholine. The most common antiviral drug is acyclovir, a synthetic nucleotide nucleoside analog derived from guanine. It works well to cure the varicella-zoster virus and the virus that causes herpes simplex (HSV), primarily HSV-1 and HSV-2. But its skin permeability is minimal. Therefore, this work aimed to use transferosomes to prepare acyclovir so that it could pass through the skin's barrier function. Objective: This study uses a 32-factorial factorial design to develop a transferosomal gel containing acyclovir through thin-film hydration method for painless acyclovir delivery services for skin disease treatment. Material and Methods: The independent variables are the amount of phospholipid (X1) and tween 80 (X2), while the dependent variables are particle size (Y1) and percentage entrapment efficiency (Y2). To create an ideal formulation, the produced transferosomes were assessed for particle size, in vitro drug release amount, and entrapment efficiency (EE%). A Carbopol 934 gel basis was prepared using the optimized acyclovir transferosome formulation, and its drug concentration, pH, spreadability, viscosity, and stability were assessed. Results: With small particles ranging from 176.6 to 324.4 nm, the produced acyclovir transferosomes had a high EE% range from 66.34 to 76.42 %. According to the in vitro release study, there is a negative correlation between in vitro release and EE%. The formulation TF5, including 1%w/w of carbopol 940, provides a superior profile of drug absorption in vitro. Consequently, acyclovir can enter the skin as transferosomes and cross the stratum corneum barrier. Conclusion: Acyclovir can be transformed into a transfersomal gel, which will improve antiviral efficacy, get over the skin's protective layer, prevent adverse oral reactions, and eventually improve patient adherence. Keywords: Transferosome, Transdermal drug delivery system, Acyclovir, 32 Fractional factorial design, Carbopol 934

Fabrication and characterisation of nabumetone transferosomal gel for effective topical delivery

Nabumetone is a lipophilic drug with a log P value of 3.2 and belongs to BCS class II due to its poor water solubility. When administered orally, it undergoes extensive first-pass metabolism, shows low bioavailability, and has unfavourable side effects that cause discomfort. Topical route has gain importance by delivering therapeutic agents via this route due to its safety and convenience of drug administration and as of there are no any gel formulations available for it. The present investigation aimed to prepare, optimise, and characterise Nabumetone-loaded transferosomes (Nb-TF) using 32 factorial designs. Transferosomes were prepared by the thin-film hydration method. The optimised formulation was incorporated into gel form (Nb-TG) and evaluated for its mechanical characteristics, in-vitro release, ex-vivo permeation, skin irritancy test, anti-inflammatory activity, and stability studies. The Nb-TF 5 transferosomal formulation was optimised based on vesicle size and entrapment efficiency and incorporated into the gel base. Both normal (Nb-gel) and transferosome-loaded (Nb-TG) gel pH was within the range of topical skin pH. The viscosities of Nb-gel and Nb-TG were 1262 ± 54 cP and 1327 ± 12 cP, respectively. The drug content of both gels was found to be 96.31 ± 1.16 and 97.18 ± 0.94, respectively. Nb-TG showed higher diffusion and drug permeation than Nb-gel. The skin irritancy test indicates that there was no sign of any edema or erythema observed. Nb-TG showed a curative and preventive anti-inflammatory effect. Gels were found stable at both refrigerator and room temperature. Nb-TFs were proven to be potential carriers for transdermal controlled delivery of Nabumetone as it has deep penetration in the dermis layer which directly goes into the systemic circulation, enhances the bioavailability and reduced toxicities.

Development of engineered transferosomal gel containing meloxicam for the treatment of osteoarthritis

.In this study, we investigated the potential of meloxicam (MLX) developed as transferosomal gel as a novel lipidic drug delivery system to address osteoarthritis (OTA), a degenerative joint disease that causes pain and stiffness. By incorporating meloxicam into a transferosomal gel, our aim was to provide a targeted and efficient delivery system capable of alleviating symptoms and slowing down the progression of OTA. Classical lipid film hydration technique was utilized to formulate different transferosomal formulations. Different transferosomal formulations were prepared by varying the molar ratio of phospholipon-90H (phosphodylcholine) to DSPE (50:50, 60:40, 70:30, 80:20, and 90:10) and per batch, 80mg of total lipid was used. The quality control parameters such as entrapment efficiency, particle size and morphology, polydispersity and surface electric charge, in vitro drug release, ex vivo permeation and stability were measured. The optimized transferosomal formulations revealed a small vesicle size (121±12nm) and greater MLX entrapment (68.98±2.3%). Transferosomes mediated gel formulation MLX34 displayed pH (6.3±0.2), viscosity (6236±12.3 cps), spreadability (13.77±1.77 gm.cm/sec) and also displayed sustained release pattern of drug release (81.76±7.87% MLX released from Carbopol-934 gel matrix in 24h). MLX34 revealed close to substantial anti-inflammatory response, with ∼81% inhibition of TNF-α in 48h. Physical stability analysis concluded that refrigerator temperature was the preferred temperature to store transferosomal gel. MLX loaded transferosomes containing gel improved the skin penetration and therefore resulted into increased inhibition of TNF-α level.

Development and Characterization of Charantin Loaded Transferosomes based Transdermal Formulation: An Effective and Patient Friendly Way for Diabetes Management

Transferosomes, marvels of scientific ingenuity, represent exquisitely optimized and ultra- deformable (ultra-flexible) lipid supramolecular aggregates, uniquely capable of traversing the mammalian skin intact. These remarkable carrier systems have harnessed the power of transdermal delivery, enabling the transport of drugs, irrespective of their molecular weight from the tiniest compounds to the most substantial ones. The incorporation of Charantin into transferosomal gel formulation holds immense promise in advancing topical therapeutics. Charantin, a bioactive compound derived from Momordica charantia, possesses potent medicinal properties with antidiabetic, anti-inflammatory, antioxidant, and antimicrobial activities. When integrated into the lipid-based transferosomal system, Charantin's efficacy is significantly amplified due to enhanced skin penetration and improved stability against degradation. The versatile nature of transferosomal gels allows for encapsulating both hydrophilic and lipophilic compounds, making it an ideal carrier for Charantin regardless of its solubility characteristics. Driven by the pursuit of excellence, the present study sought to masterfully optimize the Transferosomes to orchestrate an unparalleled symphony of enhanced skin delivery for Charantin.

Development of erlotinib-loaded nanotransferosomal gel for the topical treatment of ductal carcinoma in situ.

Aims: Thisstudy was aimed to formulate erlotinib (ERL)-loaded transferosomal gel (ERL@TG) intended for topical application for the treatment of ductal carcinoma in situ. Materials & methods: The optimized process involved athin-film hydration method to generate ERL-loaded transferosomes (ERL@TFS), which was incorporated into a carbopol gel matrix to generateERL@TG. The optimized formulation was characterized in vitro followed by cytotoxicity evaluation on MCF-7 breast cancer cell lines and acute toxicity and skin irritation studies was performed in vivo. Results: In a comparative assessment against plain ERL, ERL@TG displayed enhanced efficacy against MCF-7 cell lines, reflected in considerably lower IC50 values with anenhanced safety profile. Conclusion: Optimized ERL@TG was identified as a promising avenue for addressing ductal carcinoma in situ breast cancer.

Formulating and evaluating a gel that contains Eletriptan-loaded transferosomes

Transdermal-vesicular drug delivery systems offer various advantages over conventional drug delivery systems, such as bypassing first-pass metabolism, site-specific delivery, reduced dosing frequency, and more. The objective of the present research involves the formulation and in-vitro evaluation of Eletriptan transferosomal gel to reduce dosing frequency. Transferosomes act as vehicles for on-site drug delivery, and they are vesicular systems with a flexible membrane. By formulating this type, we can achieve a higher concentration at the site of action, thereby reducing dosing frequency.
 Fourier-transform infrared spectra revealed that there was no interaction between the drug and excipients. Transferosomal formulations were prepared by the thin-film hydration technique and were incorporated into 1.5% Carbopol gel. From the results, Formulation code-ET6, containing Lecithin: Tween-80, has higher entrapment efficiency and maximum drug release, and is hence considered the optimized formulation. Stability studies performed for optimized transferosomal gel formulations indicate that the prepared transferosomal gel has more stability at a lower temperature.
 The conclusion is that, based on the above data, it is confirmed that the prepared Eletriptan transferosomal gels can be considered as one of the promising approaches to reducing dosing frequency and maintaining drug concentration at the desired site for a longer time.
 Keywords: Transdermal drug delivery, Eletriptan, Transferosomes, Thin Film Hydration Method, Carbopol gel.

Transferosomes stabilized hydrogel incorporated rhodomyrtone-rich extract from Rhodomyrtus tomentosa leaf fortified with phosphatidylcholine for the management of skin and soft-tissue infections.

Rhodomyrtus tomentosa leaf (RT)-incorporated transferosomes were developed with lecithin and cholesterol blends with edge activators at different ratios. RT-transferosomes were characterized and employed in transferosomal gel formulations for the management of skin and soft-tissue infections. The optimized formulation entrapped up to 81.90 ± 0.31% of RT with spherical vesicles (405.3 ± 2.0nm), polydispersity index value of 0.16 ± 0.08, and zeta potential of -61.62 ± 0.86mV. Total phenolic and flavonoid contents of RT-transferosomes were 15.65 ± 0.04μg GAE/g extract and 43.13 ± 0.91μg QE/g extract, respectively. RT-transferosomes demonstrated minimum inhibitory and minimum bactericidal concentrations at 8-256 and 64-1024μg/mL, respectively. Free radical scavenging assay showed RT-transferosomes with high scavenging activity against DPPH and ABTS radicals. Moreover, RT-transferosomes demonstrated moderate activity against mushroom tyrosinase, with IC50 values of 245.32 ± 1.32μg/mL. The biocompatibility results against L929 fibroblast and Vero cells demonstrated IC50 at 7.05 ± 0.17 and 4.73 ± 0.13μg/mL, respectively. In addition, nitric oxide production significantly decreased by 6.78-88.25% following the treatment with 31.2-500ng/mL RT-transferosomes (p < 0.001). Furthermore, the freeze-thaw stability study displayed no significant change in stability in the sedimentation and pH of gel fortified with RT-transferosomes. The results suggested that RT-transferosome formulation can be effectively employed as natural biomedicines for scar prevention and the management of skin soft-tissue infections.

Formulation and Evaluation of a Transferosomal Gel of Famciclovir for Transdermal Use.

Famciclovir, the drug of choice for cold sores and recurrent genital herpes, has poor oral bioavailability and is associated with numerous side effects. The study aimed to explore the possibility of transdermal application of famciclovir through a transferosome-loaded gelling system to localize the drug at the site of application with improved penetrability, therapeutic effects, and comfort. Transferosomes of famciclovir were prepared using tween 80, phospholipid, and cholesterol. To optimize drug entrapment and the vesicular size of the transferosomes, a central composite design was employed. The optimized formulation was evaluated for physicochemical characteristics, surface morphology, and degree of deformability. The optimized product was included in the Carbopol 940 gelling system. The gel was evaluated for ex vivo permeation, skin irritation, drug deposition at various skin layers, and histopathological analysis. The design optimization yielded an optimized product (FAMOPT) of nanosized (339 nm) stable vesicles of the transferosome of famciclovir. The surface morphology analysis revealed the formation of nanovesicles without aggregation. Compatibility between the drug and excipients was established. The elasticity of the vesicles demonstrated resistance to leakage. The permeation of the drug was enhanced by 2.8 times. The gel was found to be non-irritating and non-sensitizing to the animal skin. The drug deposition at various skin layers was remarkably improved, indicating effective drug penetration. The histopathological examination further demonstrated the penetration of nano-vesiculate drugs through deeper layers of the skin. Hence, nano-vesicular famciclovir delivery is a promising alternative to conventional famciclovir delivery with enhanced local and systemic action for herpes treatment.

Formulation Development and In-Vitro Evaluation of Transferosomal Gel of Mometasone Furoate

The main aim of the study is to formulate and evaluate transferosomal gel formulation for effective topical delivery of Mometasone furoate. The transferosomes was prepared using thin film hydration technique by various proportions of Soya phosphatidylcholine, tween 80. The drug was encapsulated into eight different Transferosomal formulations from F1-F8. The optimized formulation F4 showed small particle size (152.48 nm), entrapment efficiency % EE of 87.16%, zeta potential of -32mV, 0.252 PDI and % Cumulative Drug Release of (97.14%). SEM of optimized Transferosome appeared as spherical, well identified, Unilamellar vesicles. The optimized formulation of Transferosomes was further formulated to transferosomal gel with Carbopol-940 (0.2 to 0.8% w/w), HPMC k15 (0.2 to 0.8% w/w), Propylene glycol, Triethanolamine and Isopropyl alcohol. Among these, F4 formulation with Carbopol-940 0.8%w/w transferosomal gel is the optimized transferosomal gel and showed Spreadability value 0.229±0.01gm.cm/sec, pH value 5.8. The actual drug content of the Transferosomal gel was found to be 98.90%, which represents good content uniformity. The viscosity of optimized Transferosomal gel was found to 55417cps. The percentage drug release for Transferosomal gel was 98.22%. And the formulation was stable throughout the stability studies. This research suggests that Mometasone Furoate loaded transferosomal gel can be potentially used as a transdermal drug delivery system for effective topical delivery.&#x0D; Keywords: Mometasone Furoate, Transfersomes, Soya phosphatidyl choline and Tween 80.

Formulation and In-Vitro Evaluation of Gabapentin Loaded Transferosomal Gel

Gabapentin is an anticonvulsant which is primarily used to treat peripheral neuropathy. It belongs to class III drugs having High solubility and low permeability. The present study is carried out on formulation and invitro evaluation of Gabapentin Transferosomal gel by using various surfactants, polymers. The Transferosomes were prepared by thin film hydration technique. Different proportions of surfactants have been utilized such as span 80 and tween 80. 8 distinctive formulations of Gabapentin transferosomes had been formulated and evaluated for parameters like FTIR, Organoleptic evaluation, Drug content, Entrapment efficiency, Invitro diffusion studies, SEM, Zeta potential and particle size analysis, pH, Spreadability, Viscosity, Stability testing and Kinetic studies. The optimized formulation Gf6 confirmed Entrapment efficiency of 86.54%, Drug content 96.11% Zeta potential of -31.64Mv, particle size of 164.2nm, In-vitro drug release ranging from (75.15- 89.37%). The drug release data of selected formulation confirmed desirable fit into Zero order and Peppas release Kinetics. Overall, it can be concluded that the transferosomal gel can overcome problems associated with convectional routes of drug delivery.&#x0D; Keywords: Gabapentin, Transferosomes, Edge activators, Thin film hydration method.

Formulation and in-vitro Evaluation of Baclofen loaded Transferosomal Gel

Baclofen is a class of medications called skeletal muscle relaxant. It is a class III drug having low solubility and high permeability used in treating multiple sclerosis symptoms such as spasticity, stiffness, and pain. The current study involves the development and in-vitro evaluation of a Baclofen-loaded transfersomal gel to reduce dosage frequency. Drug and excipient interactions were not detected in the FTIR spectra. Hand shaking modified thin film hydration method was used to developed transfersome formulations, which then consolidated at 0.5% carbopol gel. Optimized BF7 formulation provides higher Entapment efficiency and maximum drug delivery. The prepared formulation had been examined for FTIR, Organoleptic evaluation, Viscosity, Spread-ability, Entrapment Efficacy, Drug content, SEM analysis, Particle size, Zeta potential, Stability testing, and other parameters. The optimised formulation BF7 confirmed Entapment Efficiency ranging from 80.04 to 87.42%, Drug content ranging from 90.26 -95.37%, Vesicle Size of 167.8nm &amp; In-vitro diffusion of 97.48%. The drug release data from the chosen gel demonstrated a good fit with the Higuchis and Zero order release kinetics.&#x0D; Keywords: Transferosomes, vesicular drug delivery system, Thin film hydration method

Development and Evaluation of Curcumin-based Transferosomal Gel for Wound Healing

Background: Recently, transferosomes have been discovered to have the potential for transdermal delivery. Curcumin is a bioactive molecule with anti-inflammatory and antioxidant properties, but it has low water solubility and poor skin absorption. The biological response to damage caused by diverse stimuli is known as the inflammatory process. Cyclodextrins are cyclic (-1, 4)-linked oligosaccharides of -D-glucopyranose with a hydrophilic outer surface and a hydrophobic center cavity. Aim: The aim of the study was to develop a curcumin-loaded transferosomal gel to improve the wound healing process. The study has focused on advancing the area of traditional medicine in the field of pharmaceutics by using curcumin in the form of transferosomes to enhance wound healing. Method: Firstly, curcumin was used to synthesize the transferosomes. Secondly, the transferosomes were converted into a transferosomal gel as an alternative for wound healing. Characterization and in vivo investigation were carried out on female Swiss mice. Results: Unpaired Student’s t-test was used to determine the statistical significance at p &lt; 0.5 using UV exposure schedules. All values have been expressed as mean ± SEM calculated by ANOVA with a significant difference among means at P &lt; 0.05. Conclusion: The study has indicated curcumin to be successfully entrapped in transferosomes in order to formulate the gel with powerful wound healing properties.

Preparation and formula optimization of cephalexin loaded transferosomal gel by QbD to enhance the transdermal delivery: In vitro, ex vivo and in vivo study

Preparation and formula optimization of cephalexin loaded transferosomal gel by QbD to enhance the transdermal delivery: In vitro, ex vivo and in vivo study

Development and evaluation of the novel chitosan-based 1% clindamycin &amp; 2.5% benzoyl peroxide transferosomal gel for topical acne treatment

Development and evaluation of the novel chitosan-based 1% clindamycin &amp; 2.5% benzoyl peroxide transferosomal gel for topical acne treatment

Curcumin Transferosome-Loaded Thermosensitive Intranasal in situ Gel as Prospective Antiviral Therapy for SARS-Cov-2.

Immunomodulatory and broad-spectrum antiviral activities have motivated the evaluation of curcumin for Coronavirus infection 2019 (COVID-19) management. Inadequate bioavailability is the main impediment to the therapeutic effects of oral Cur. This study aimed to develop an optimal curcumin transferosome-loaded thermosensitive in situ gel to improve its delivery to the lungs. Transferosomes were developed by using 33 screening layouts. The phospholipid concentration as well as the concentration and type of surfactant were considered independent variables. The entrapment efficiency (EE%), size, surface charge, and polydispersity index (PDI) were regarded as dependent factors. A cold technique was employed to develop thermosensitive in-situ gels. Optimized transferosomes were loaded onto the selected gels. The produced gel was assessed based on shape attributes, ex vivo permeability enhancement, and the safety of the nasal mucosa. The in vitro cytotoxicity, antiviral cytopathic effect, and plaque assay (CV/CPE/Plaque activity), and in vivo performance were evaluated after intranasal administration in experimental rabbits. The optimized preparation displayed a particle size of 664.3 ± 69.3 nm, EE% of 82.8 ± 0.02%, ZP of -11.23 ± 2.5 mV, and PDI of 0.6 ± 0.03. The in vitro curcumin release from the optimized transferosomal gel was markedly improved compared with that of the free drug-loaded gel. An ex vivo permeation study revealed a significant improvement (2.58-fold) in drug permeability across nasal tissues of sheep. Histopathological screening confirmed the safety of these preparations. This formulation showed high antiviral activity against SARS-CoV-2 at reduced concentrations. High relative bioavailability (226.45%) was attained after the formula intranasally administered to rabbits compared to the free drug in-situ gel. The curcumin transferosome gel displayed a relatively high lung accumulation after intranasal administration. This study provides a promising formulation for the antiviral treatment of COVID-19 patients, which can be evaluated further in preclinical and clinical studies.

Transferosomal gel for transdermal delivery of insulin: Formulation development and ex vivo permeation study

The study was to develop a transdermal formulation of insulin, determine its pharmaceutical characteristics, and finally test its efficacy. In the current study - Transfersomes were selected as the carrier system for insulin. The transfersomes were produced by the hand-shaking method using soy lecithin phospholipid and sodium deoxycholate as the objective of the surfactant. The prepared transfersomes were subjected to characterization with optical microscopy and scanning electron microscope to estimate the shape and size of transfersomes respectively. In addition, the physical and drug-excipient interaction studies were carried out and the transfersomes were also studied for the insulin entrapment efficiency.Results of the study showed the shape of the transfersomes was well defined and spherical. The mean size of transfersomes was estimated to be 130 ​nm The transfersomes were found to be stable over a period of four weeks. The insulin entrapment efficiency of the transfersomes was estimated to be 87.3%. The ex-vivo skin permeation study employing goat ear skin with the transfersomes hydrogel revealed that there was a slow and sustained release of insulin till 180 ​min. From the above study, it may be concluded that transfersomes are suitable carriers of insulin across biological membranes.

Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies.

Numerous neurological disorders have a pathophysiology that involves an increase in free radical production in the brain. Quercetin (QER) is a nutraceutical compound that shields the brain against oxidative stress-induced neurodegeneration. Nonetheless, its low oral bioavailability diminishes brain delivery. Therefore, the current study aimed to formulate QER-loaded transferosomal nanovesicles (QER-TFS) in situ gel for QER brain delivery via the intranasal route. This study explored the impacts of lipid amount, edge activator (EA) amount, and EA type on vesicle diameter, entrapment, and cumulative amount permeated through nasal mucosa (24 h). The optimum formulation was then integrated into a thermosensitive gel after its physical and morphological characteristics were assessed. Assessments of the optimized QER-TFS showed nanometric vesicles (171.4 ± 3.4 nm) with spherical shapes and adequate entrapment efficiency (78.2 ± 2.8%). The results of short-term stability and high zeta potential value (-32.6 ± 1.4 mV) of QER-TFS confirmed their high stability. Compared with the QER solution, the optimized QER-TFS in situ gel formulation exhibited sustained release behavior and augmented nasal mucosa permeability. CT scanning of rat brains demonstrated the buildup of gold nanoparticles (GNPs) in the brains of all treatment groups, with a greater level of GNPs noted in the rats given the transferosomal gel. Additionally, in vitro studies on PCS-200-014 cells revealed minimal cytotoxicity of QER-TFS in situ gel. Based on these results, the developed transferosomal nanovesicles may be a suitable nanocarrier for QER brain targeting through the intranasal route.

FORMULATION AND EVALUATION OF TRAMADOL HYDROCHLORIDE LOADED TRANSFEROSOMAL GEL BY THIN FILM HYDRATION TECHNIQUE

Objective(s): The current studys goal is to develop and test a tramadol hydrochloride transdermal gel based on vesicular drug delivery approaches. Materials and methods: Transferosomes were chosen as the colloidal carrier for tramadol hydrochloride transdermal gel preparation. Thin film hydration was used to create transferosomes. The obtained transferosomes were characterised for drug content, vesicular diameter, zeta potential, entrapment efficiency, invitro drug release studies. Results: T5 (made via thin film hydration and comprising a soya lecithin: Tween 60 ratio of 1:2.5) was deemed the best transferosome formulation due to its 274.2nm mean vesicular diameter, -29.5 mV zeta potential, 93.9% drug content, 97% entrapment efficiency, and 92.7% sustained drug release after 12 hours. The T5 formulation was included into the gel. There was a comparison between plain gel and transfersomal gel. Transfersomal gel was rated superior to the other gels due to its higher drug concentration (91%), spreadability (18.35 g.cm/sec), pH (6.9), and sustained drug release profile over 12 hours. Conclusion: By comparing transferosomal gel with plain gel transferosomal gel indicated better results than plain gel.