Liposomal Gel Formulations Research Articles

Preparation and evaluation of liposomal gel containing Neolamarckia cadamba leaves extract for anti-inflammatory activity

The objective of present research work is to develop liposomes as a carrier system for methanolic extract, its incorporation in to gel formulations and to characterize the prepared and develop liposomal gel formulation. Formulation was carried out by thin film technique. Scanning electron micrograph of the prepared nanosponges at 50.00 kx magnification showed that the liposome was porous with a smooth surface morphology and spherical shape. The porous nature of liposome was clearly observed in the SEM images. Particle size and zeta potential was determined by Malvern Zeta sizer. The particle size analysis confirmed that the prepared sample were in the nanometer range. Average particle size obtained for the formulations F1 to F5 were 162.7 nm to 195.6 nm. Zeta potential values of liposome indicated that the formulated liposomes are stable. The amount of drug being entrapped in liposome was calculated and all the prepared liposome was found to possess very high entrapment efficiency. The viscosity of liposome loaded gel is found to 6842±0.32cps. The pH of liposome loaded gel is 6.3 and spreadability is 12.11, indicating that liposome loaded gel has high release and permeability. The in vitro anti-inflammatory effect of Neolamarckia cadamba extract was evaluated against denaturation of egg albumin. The present findings exhibited a concentration dependent inhibition of protein (albumin) denaturation by Neolamarckia cadamba throughout the concentration range of 20-100μg/ml. Diclofenac sodium (at the concentration range of 20-100 μg/ml) was used as reference drug which also exhibited concentration dependent inhibition of protein denaturation; however, the effect of diclofenac sodium was found to be less active when compared with extract name. Moreover, the results demonstrated that the liposome-based drug delivery approach could be a valuable tool to improve the therapeutic efficacy of phytochemicals by improving their absorption, and bioavailability via altering their physicochemical and release properties. Keywords: Liposomes, Neolamarckia cadamba, Qualitative phytochemical screening, Thin film technique, In vitro anti-inflammatory activity.

Design, Optimization, and Characterization of Zolmitriptan Loaded Liposomal Gels for Intranasal delivery for acute migraine therapy

Zolmitriptan is the primary drug for the treatment of Migraine. However, the bioavailability of the drug is low and requires repetitive administration leading to side effects. Zolmitriptan's bioavailability can be improved by incorporating it into liposomes as a topical intranasal gel. The formulation was developed using a Central composite design employing a response surface approach. The new formulations were tested for particle size, shape, drug entrapment efficiency, and in vitro drug release. Permeation experiments and histopathology in rats were also conducted to determine the formulation's safety. The vesicle size was found to be in the range of 103.82±7.16 to 694.38±1.02 nm, zeta potential --19.28 to -32.8 mV, Entrapment Efficiency from 55.49±1.37 to 99.12±0.36 %, and cumulative drug release from 59.71±6.94 to 99.38±0.13 % respectively. In-vitro drug release of G1 and G3 gel formulations showed a non-Fickian released pattern during the studies. A comparison of the permeation coefficient of G1 (0.539 μg/cm2) and G3 (5.3 μg/cm2) showed a slight variation in the drug release rate after 24 hrs. For the liposomal gel and its solution, we found a significant difference in drug penetration of p0.05 after 12 hours compared to the control gel. There were substantial differences in bioavailability and pharmacokinetics between the optimal Liposomal Gel Formulation and other formulations, including the drug solution, liposomal suspension, and optimized formulation F12. The liposomal gel is non-irritating and safe for topical administration by histopathological investigations. Therefore, the study demonstrated that Zolmitriptan Liposomal gel has better efficacy, good tolerability, and enhanced bioavailability, making it an optimal treatment for acute Migraine.

Simvastatin-Encapsulated Topical Liposomal Gel for Augmented Wound Healing: Optimization Using the Box-Behnken Model, Evaluations, and In Vivo Studies.

Statins function beyond regulating cholesterol and, when administered systemically, can promote wound healing. However, studies have yet to explore the topical use of statins for wound healing. The present study demonstrated the topical administration of SIM and aimed to formulate, evaluate, and optimize Simvastatin (SIM)-encapsulated liposome gel carrier systems to facilitate successful topical wound healing. Liposomes containing SIM were formulated and optimized via a response surface methodology (RSM) using the thin-film hydration method. The effects of formulation variables, including the 1,2-dioleoyloxy-3-trimethylammoniumpropan (DOTAP) concentration, Span 80 concentration, and cholesterol concentration, on zeta potential (mV), entrapment efficacy (%), and particle size (nm) were studied. The optimized liposome formulation (F-07) exhibited a zeta potential value of 16.56 ± 2.51 mV, revealing robust stability and a high SIM encapsulation efficiency of 95.6 ± 4.2%, whereas its particle size of 190.3 ± 3.3 nm confirmed its stability and structural integrity. The optimized liposome gel demonstrated pseudoplastic flow behavior. This property is advantageous in topical drug delivery systems because of its ease of application, improved spreadability, and enhanced penetration, demonstrating prolonged SIM release. The assessment of the wound healing efficacy of the optimized liposomal gel formulation demonstrated a substantial decrease in wound size in mice on the sixteenth day post-wounding. These findings suggest that the use of liposomal gels is a potential drug delivery strategy for incorporating SIM, thereby augmenting its effectiveness in promoting wound healing.

Preparation and Evaluation of Diclofenac Sodium Loaded Liposomal Hydrogel in the Treatment of Rheumatoid Arthritis

In the present research, it was proposed to provide topical delivery of diclofenac sodium. Diclofenac sodium will be encapsulate in liposome and further loaded into a hydrogel and delivered through topical route. The lipid film hydration approach was used to create diclofenac sodium liposomes, which were then characterised by vesicle size, zeta potential, and entrapment effectiveness. The pH of the generated liposomal gels was within the permissible range of 7.0-7.2. The spreadability of the gels was assessed using slip and drag characteristics and was found to be between 10.45 and 12.32 gm.cm/sec. F1, F2, and F3 spreadabilities were determined to be 10.45±0.075,12.32±0.042 and 11.75±0.049 gm.cm/sec, respectively. The viscosities for F1, F2, and F3 were determined to be 1870±25 cps, 1895±33 cps, and 1875±21 cps, respectively. The percentage of cumulative medication (diclofenac sodium) released from F1, F2, and F3 liposomal gel formulations was 98.15%±17, 98.72%±2.4 and 96.27%±2.7 respectively.

Clinical evaluation of liposome-based gel formulation containing glycolic acid for the treatment of photodamaged skin

Background: Long contact of UV causes skin damage. Glycolic acid (GA) as an alpha hydroxy acid is used to treat photodamaged skin. However, GA leads to side effects including; burning, erythema and peeling. Purpose: The aim of this study was to develop a controlled delivery systems loading GA in order to increasing its efficacy and lowering its side effects. Methods: Liposomes were evaluated for encapsulation efficiency, size and morphology. Optimized formulation was dispersed in HPMC gel bases and drug release kinetics were also studied. Clinical efficacy and safety of GA-loaded liposomal gel and GA gel formulation were evaluated in patients with photodamaged skin. Results: The EE% and average particle size of liposomes were 64 ±2.1 % and 317±3.6 nm, respectively. SEM image showed that liposomes were spherical in shape. In vitro release kinetics of GA from both formulations followed Weibull model. Clinical evaluation revealed that GA-loaded liposomal gel was more effective than GA gel formulation. Treatment with GA-loaded liposomal gel resulted in a statistically significant reduction in the scores of hyperpigmentation, fine wrinkling and lentigines. Moreover, liposomal gel formulation was able to minimize side effects of GA. Conclusion: According to the obtained results, the liposome-based gel formulation can be used as potential drug delivery system to enhance permeation of GA through skin layers and also reduce its side effects.

Development of Liposomal Encapsulated Silver Sulfadiazine Gel for Burn Therapy

The aim of the present study was to formulate stable silver sulfadiazine (SSD) liposomal gel suitable for topical delivery with a view to increase bactericidal activity in burn therapy. SSD liposomes were formulated using thin film hydration technique. A 23 factorial design was utilized to study the effect of the molar ratio of lipid: cholesterol (X1), drug concentration (X2) and hydration volume on Encapsulation efficiency (EE%) and vesicle size. Selected batch of liposome was incorporated in to PVPK-30 and HPMCK4M gel base to prepare the liposomal gel formulation, which was evaluated for in-vitro release and in-vivo study. It was evident from the derived polynomial equations and constructed contour plot, an increase in the level of X1 and a decrease in the X2 lead to an increase in EE% and increase in vesicle size. Each of the prepared liposomal gel formulation significantly improved (P<0.05) cumulative amount of drug release owing to the influence of the gel matrix. Among the liposomal gel formulation, L6 (prepared at high level of X1 and low level of X2) showed best release may be due to efficient hydration of the film and more total amount of drug entrapped. In-vivo studies revealed that a liposomal gel containing 0.5% SSD was more effective in wound healing compared to marketed cream.

Localized delivery of Erlotinib using liposomal gel formulations for the treatment of oral squamous cell carcinoma

Oral cancer accounts for more than 350,000 cases worldwide with 90% of them being oral squamous cell carcinomas (OSCC). The current treatment modalities of chemoradiation have poor outcomes along with harmful effects to neighbouring healthy tissues. The present study aimed to deliver Erlotinib (ERB), locally at the site of tumor arising in the oral cavity. ERB was encapsulated in liposomal formulations (ERB Lipo) and optimized using full factorial, 32 experimental design. The optimized batch was then coated with chitosan to obtain CS-ERB Lipo and were characterized further. Both liposomal ERB formulations had size <200 nm and PDI < 0.4. Zeta potential was upto −50 mV for ERB Lipo and upto +25 mV for CS-ERB Lipo indicating stable formulation. Liposomal formulations were freeze dried and loaded into gel to study in-vitro release and chemotherapeutic evaluation. CS-ERB Lipo showed sustained release upto 36 h from gel as compared to control formulation. In-vitro cell viability studies showed potent anti-cancer activity on KB-cells. In-vivo studies showed better pharmacological efficacy in terms of tumor volume reduction for ERB Lipo gel (49.19%) and CS-ERB Lipo gel (55.27%) as compared to plain ERB Gel (38.88%) applied locally. Histology also revealed that formulation could alleviate dysplasia condition to hyperplasia. The locoregional therapy of ERB Lipo gel and CS-ERB Lipo gel thus show promising outcome in improving pre-malignant and early-stage oral cavity cancers.

BOX-BEHNKEN DESIGN OPTIMIZATION OF SALICYLIC ACID LOADED LIPOSOMAL GEL FORMULATION FOR TREATMENT OF FOOT CORN

Objective: The present research is aimed to design and optimize a liposomal gel formulation of salicylic acid (SA) for enhanced drug permeation, higher skin drug retention, sustained release drug delivery and reduced side effects in the effective treatment of foot corn. Methods: Formulation designing and optimization of SA-loaded liposomes was done by box-Behnken experimental design using the three-factor, three-level approach. Phospholipid content, cholesterol content and drug content were selected as independent variables; while the critical quality attributes (CQAs) of liposomal formulation like particle size, PDI, zeta potential, entrapment efficiency and cumulative % drug release were considered as response variables. The SA-loaded liposomes were prepared by ethanol injection method and were characterized for desired CQAs. Finally, topical gel formulation of SA-loaded liposomes was developed and evaluated for drug content, homogeneity, spreadability, in vitro drug release, drug release kinetics, ex-vivo drug permeation and skin retention properties. Results: The particle size, PDI, zeta potential, entrapment efficiency and cumulative % drug release of SA-loaded liposomes was found to be 261.2 nm, 0.28, 0.7 mV, 57.53% and 99.57%, respectively. Developed topical gel formulation of SA-loaded liposomes exhibited a sustained drug release profile (64.48% cumulative release over 360 min) following Higuchi model kinetics. The developed formulation showed almost 2-fold enhanced drug permeation (i.e., 26.50%) and more than 2-fold higher drug retention (i.e., 10.90%) on porcine ear skin as compared to the plain salicylic acid gel. Conclusion: The SA-loaded liposomes and developed topical gel formulation possessed all desired CQAs. The in vitro drug release kinetics, ex-vivo drug permeation and skin retention studies confirmed the suitability of the developed formulation for topical application in the effective treatment of foot corn.

UPLC-MS/MS Method Development for Simultaneous Estimation of Diclofenac and Resveratrol-Loaded Liposomal Gel Formulation in Mice Skin Model: Application to Dermatokinetic Study.

The current research work describes the development of a simple, fast, sensitive and efficient bioanalytical UPLC/MS-MS method for the simultaneous estimation of diclofenac and resveratrol in mice skin samples. Quetiapine was used as an internal standard (IS). Analytical separation was performed on ACQUITY UPLC C18 Column (2.1 × 100mm; 1.7μm) using ammonium acetate (5mM) in water and methanol (B) with isocratic elution at ratio of (50, 50v/v) and flow rate of 0.4mL/min. The duration of separation was maintained for 3min. Electrospray ionization mass spectrometry in a positive and negative ionization mode was used for detection. Selective ion mode monitoring was used for the quantification of m/z 296.025> 249.93 for diclofenac, m/z 229.09 > 143.03 for resveratrol and MRM/ES+ve mode applied in m/z 384.25> 253.189 for IS transitions from parent to daughter ion. The lower detection and quantification limits were accomplished, and precision (repeatability and intermediate precision) with a coefficient of variation below 10% produced satisfactory results. The developed bioanalytical method was found to be useful for its suitability for the dermatokinetic evaluation of treatments through rat skin. Improvement in AUC (1.58-fold for diclofenac and 1.60-fold for resveratrol) and t1/2 in the dermis (2.13 for diclofenac and 2.21-fold for resveratrol) followed by epidermis was observed for diclofenac and resveratrol-loaded liposomal gel formulation over the conventional gel. Overall, the developed method for the dermatokinetic studies of the above-mentioned dual drugs-loaded liposome gel was found to be reproducible and effective for bioanalytical.

Formulation and Evaluation of Natural Liposomal Gel for Breast Cancer

As per world health organization (WHO) report in 2020 about 2.3 million were diagnosed globally with breast cancer and around 6.85 lacs death occurs globally due to breast cancer. In such case usage of natural anticancer remedies can provide beneficial results, but unfortunately natural drugs are not being practically useful due to trifling bioavailability and unempirical data of effectiveness. In current study, liposomal gels were formulated by using liposomes entrapped with natural compound like seasamine, aloe-emodin, gallic acid, catechin, butein, 6-gingerol and curcumin as active drugs. Liposomal gels were formulated using carbopol (1.5 % w/w) with variable concentration of propylene glycol, in another formulation mixture 1 % w/w HPMC, 1 % w/w microcrystalline cellulose and 3 % w/w sodium alginate were also used. From characterization results of all of the above formulations, formulation with 1.5 % w/w carbopol and 5 % w/w propylene glycol has shown significant release of active drugs. In addition to this penetration effect of propylene glycol was also accessed for topical liposome gel formulation; the data reveals that propylene glycol has no significant penetration boosting impact with liposomal gel formulation.

DEVELOPMENT AND IN-VITRO CHARACTERIZATION OF LIPOSOMAL GEL OF BIFONAZOLE FOR TOPICAL USE

The main objective of this study is to prepare and evaluate liposomes as a carrier for bifonazole. Liposomes are colloidal particles designed as concentric biomolecular layers that are capable of encapsulating drugs. Liposomes of soya lecithin and cholesterol were prepared in ten batches (L1- L10) with different ratio using thin film hydration technique. Prepared liposomes were evaluated for entrapment efficiency and particle size analysis. Liposomal gel formulations of prepared liposomes were formulated in six batches (L9F1- L9F6) and evaluated for drug content, in-vitro drug release study, particle size, zeta potential, polydispersity index (PDI) and stability study were performed. The entrapment efficiency, particle size, zeta potential and PDI of all liposome vesicle preparations were analyzed and it was found that the batch L9 liposome vesicles produced the entrapment efficiency 76.52 ± 0.175, particle size 119.1 nm, zeta potential -0.4, and PDI was found to be 0.406. Liposomal gel formulation was prepared. The drug content, in-vitro drug release study and stability study of all six batches of liposomal gel formulation were analyzed, and it was found that the L9F3 formulation shows better drug content, in-vitro drug release and stability at 5°C ± 2°C among all the formulations. Evaluation of prepared liposomal gel formulations was performed. After comparing all formulations of evaluation results on the basis of drug content and, in-vitro drug release and stability study, batch L9F3 formulation was considered as the best formulation.

Formulation and Evaluation of Hydrogels containing Liposomes Entrapped with Antifungal Agent

Background: The main aim of the present study was to formulate and evaluate prolonged release Fluconazole liposomal gel for the transdermal delivery. Fluconazole, α-(2.4-diflurofenil)-α-(1H-triazole-1-methyl)-1H-1, 2, 4-triazole-1-ethanol, is a class of antifungal of triazole. It shows the action against species of Candida sp., and it is specified in cases of or pharyngeal candidiasis, esophageal, vaginal, and deep infection. Materials and Method: Fluconazole liposomal gel was prepared by thin film hydration method using phosphatidyl choline and cholesterol. Liposomes were characterized for entrapment efficiency, particle size, and surface charge. Liposomes were then dispersed into a Carbopol gel base to form liposomal gel and evaluated for drug content, pH, spreadability, viscosity and in-vitro drug release. Results: The results indicated that concentration of cholesterol in the formulations affected the particle size and entrapment efficiency. When the concentration of cholesterol increased particle size was also increased but decrease in entrapment efficiency. The viscosity of Fluconazole liposomal gel decreases with increasing rate of shear. Hence it was showed that with non-Newtonian flow. In-vitro diffusion studies were carried out using cellophane membrane, results showed that liposomal gel formulation F1 (91.36%) showed highest cumulative percent of drug release and formulation F8 (76.98%) showed lowest cumulative percent of drug release. Conclusion: Therefore, Fluconazole liposomal gel sustained the drug release for the longer duration, hence decreases the number of application of drugs and also improves patient compliance.

Deformable Liposomal Hydrogel for Dermal and Transdermal Delivery of Meloxicam.

Background and AimMeloxicam (MX) is a potent hydrophobic non-steroidal anti-inflammatory drug used to reduce inflammation and pain. However, its oral dosage form can cause many adverse gastrointestinal effects. In the present study, a poloxamer P407 based hydrogel system containing transfersomes or flavosomes has been prepared as a potential therapeutic vehicle for the topical delivery of MX.MethodsIn this study, MX was encapsulated in conventional liposomes, transfersomes, and flavosomes. The obtained liposomal vesicles were characterized in terms of size, drug entrapment efficiency, zeta potential, and stability. These MX-loaded liposomal formulations were further incorporated into a poloxamer P407 gel and evaluated using rheological properties, a stability study and an ex vivo permeation study through human cadaver skin by both HPLC analysis and confocal laser scanning microscopy (CLSM).ResultsThe developed deformable liposomes exhibited homogeneous vesicle sizes less than 120 nm with a higher entrapment efficiency as compared to conventional liposomes. The deformable liposomal gel formulations showed improved permeability compared to a conventional liposomal gel and a liposome-free gel. The enhancement effect was also clearly visible by CLSM.ConclusionThese deformable liposomal hydrogel formulations can be a promising alternative to conventional oral delivery of MX by topical administration. Notably, flavosome-loaded gel formulations displayed the highest permeability through the deeper layers of the skin and shortened lag time, indicating a potential faster on-site pain relief and anti-inflammatory effect.

Multifaceted targeting of cationic liposomes via co-delivery of anti-IL-17 siRNA and corticosteroid for topical treatment of psoriasis

Psoriasis is a chronic autoimmune disorder that affects the skin to alter its structure and physiology and express the phenotypic function of abnormal epidermal cell growth through a cascade of molecular, and cellular intervention. The histological changes in skin include inflammation, scaling, hyperproliferation of epidermis resulting in thickening of the skin, under the influence of altered immunopathogenesis. The zone of activity for the therapeutic targeting of psoriasis is viable epidermis involving various cellular events regulating the whole progression of the disease manifestation. Therefore, therapeutic targeting of psoriasis through the systemic route would be imprecise and associated with numerous side effects. Small interfering RNA (siRNA) molecules have emerged as a powerful class of therapeutics for treating psoriasis. However, successful targeted delivery of necked siRNA into the skin is hampered due to physicochemical features, proneness to enzymatic degradation, and unavailability of effective delivery carriers. The steroidal medications are the most preferred choice among existing conventional topical formulations; however, they also have their drawbacks like poor aqueous solubility, deprived drug penetration across the skin, reduced half-life, dose-dependent side effects, and reduced patient compliance. In the present study, we hypothesize the development of a liposomal gel formulation for co-delivery of siRNA (siRNA against IL-17A) and a steroidal drug (Clobetasol propionate) to target different pathogenic events of psoriasis leading to the accomplishment of synergistic therapeutic effect. Since a sequence of events simultaneously occurs during the pathogenesis of psoriasis, synergistic blends of siRNA and corticosteroid would ensure a multi-targeted treatment that would act through a diverse range of mechanisms, ultimately leading to the enhancement of therapeutic effect. Therefore, exploiting the full therapeutic potential of these therapeutics. Thus, the present work suggests a novel, innovative, and promising idea for accomplishing effective treatment of psoriasis.

Development and Characterization of Tacrolimus Liposomal Gel for Industrial Application

Objective: The objective of the present study was to prepare tacrolimus liposomal gel formulations using ethanolic injection technique for efficacious and cost-effective treatment of atopic dermatitis. Methods: The liposomes were prepared using ethanolic injection technique at the drug concentration of 0.1% w/v and optimized by varying the lipid component/ cholesterol ratio and by monitoring particle size, polydispersity and entrapment efficiency. The optimized composition was incorporated into 0.5% Carbopol Ultrez 10 gel for topical application. The developed liposomal gel was evaluated with respect to physicochemical parameters such as pH, viscosity, rheometery and spreadability. Stability study was performed at different temperatures (4°C, 25°C and 40°C) to evaluate the long-term stability. In vitro permeation of tacrolimus gel was studied using freshly excised rat skin on Franz diffusion cell. The therapeutic efficacy study was performed on allergic contact dermatitis model in rats. Results: Stable tacrolimus liposomal gel was successfully formulated using ethanolic injection technique. In-vitro permeation study indicated higher release of the drug (69.7%) as compared to free drug in hydroalcoholic solution (32.8%) and marketed ointment (63.7%). The formulation also showed shear thinning performance, which is a required property of topical formulation. The therapeutic efficacy study in rats indicated that liposomal gel containing 0.1% tacrolimus exhibited better activity as compared to 0.1% marketed tacrolimus ointment. Conclusion: The study indicated that tacrolimus can be effectively incorporated in liposomes by commercially viable rapid ethanolic injection method and can be more efficient for the treatment of atopic dermatitis.

FORMULATION AND EVALUATION OF LIPOSOMAL GEL CONTAINING EXTRACT OF PIPRINE

Objective: The objective of present research work is to develop Liposomes as a carrier system for 70% Hydroalcoholic extract, its incorporation in to gel formulations and to characterize the prepared and develop Liposomal gel formulation. There are many reports revealing the pharmacological potential of Piper Nigrum.&#x0D; Methods: Cholestrol in various weight ratios were dissolved in 10 ml of Methanol: Chloroform (1:1) ratio used as a solvent. The extract solution was taken in a 500 ml round bottom flask. The flask was rotated in rotary flash evaporator at 40 rpm for 20 min in the thermostatically controlled water bath at 40 °C under vacuum 240 mmHg. The solvent was slowly removed by this process, and a very thin film of dry lipids was formed on the flask. The dry lipid film was slowly hydrated with 10 ml of Saline Phosphate Buffer pH 7.4 containing Insulin Drug. The flask was once again rotated at the same speed as before and at room temperature for 2 hr. The liposomal was left to overnight at 4°C, full lipid hydration.&#x0D; Results: This study was done for herbal formulations used for topical delivery of therapeutic agents at the time of injury to accelerate skin repair in the shortest time possible, with minimal pain. Plant Piper Nigrum. Family Piperaceac is extensively used.&#x0D; Conclusion: The present study revealed liposomal gel as an efficient carrier for herbal extract. Keywords: Piperine, Gel, Herbal extract, Liposomes, Liposomal gel.

Enhanced penetration and improved therapeutic efficacy of bexarotene via topical liposomal gel in imiquimod induced psoriatic plaque model in BALB/c mice

Bexarotene is a retinoid X receptor agonist originally approved for anti-cancer activity, which was found to have anti-psoriatic activity in recent studies. However, its poor water solubility and high log P makes it difficult to deliver via topical route. Incorporation of bexarotene into liposome will address this issue by improving the solubility and permeability of the drug. In this study, bexarotene liposomes were prepared by optimization of different parameters including lipid to cholesterol ratio, sonication time, percent drug loading and entrapment efficiency. Optimized liposomes of particle size and size distribution (67.8.2 ± 7.15 nm, 0.26 ± 0.02 PDI) with greater than 90% entrapment efficiency were incorporated into gel and tested for rheological behaviour and drug release. Dermal uptake studies of dye loaded liposomes showed improved penetration compared to plain dye. Pharmacodynamic studies performed by employing imiquimod induced psoriatic plaque model in BALB/c mice confirmed effective reversal of psoriasis from liposomal bexarotene as indicated by reduced scaling, inflammation without any toxicity. Further histopathological and cytokine level changes also confirmed the recovery of animals treated with liposomal gel formulation. These results concluded that, formulating bexarotene into liposomal gel improved anti-psoriatic efficacy of the drug.

Liposome-based combination therapy for acne treatment

Acne vulgaris is one of the most common chronic diseases worldwide with the high prevalence ratio of about 80–85% in patients who are in puberty period. For the treatment options, many conventional dosage forms are available; however, existing limitations of systemic administration of drugs (oral antibiotics), such as adverse events and resistance, led for seek of new formulation options. In this study, liposomes containing tetracycline HCl and tretinoin were prepared by the film formation method. In vitro characterization studies revealed that liposomes (111.10 ± 8.02 nm; P.D.I.=0.198 ± 0.03; Z.P.=25.83 ± 0.40 mV) with an encapsulation efficiency more than 80% for both APIs were formulated. In order to maintain a suitable viscosity for topical application, optimized liposomal formulations were dispersed in carbopol-based gel. In vitro release of APIs was sustained for 24 hours with released amounts of 56.44% and 58.44% for tetracycline HCl and tretinoin, respectively. Stability evaluation of both liposomes and liposomes in hydrogels was investigated for 6 months at 4 °C and 25 °C; and no statistically significant change was observed in terms of particle size, zeta potential, encapsulation efficiency, appearance, pH, and viscosity. Cytotoxicity tests confirmed the nontoxic structure of liposomal gel formulations on mice fibroblast cells. In addition, antibacterial efficacy has been proven with Staphylococcus aureus and Streptococcus epidermidis strains as well as the effect on biofilm formation and eradication. As a result, we hereby presented a new combination drug product, which consists of dual active ingredients having comedolytic and bacteriostatic effects in a single, safe, and stable liposome formulation.

Formulation development, characterization and assessment of In-Vitro antifungal efficacy against Candida albicans of diallyl disulphide liposomal gel using 32 factorial design

Objective: The aim of this study was to develop the diallyl disulphide (DADS) liposomal dispersion and further the dispersion was to formulate into gel.&#x0D; Methods: The DADS liposomal system was developed using thin film hydration method. 32 factorial design was employed to study the effect of various factors to obtain the optimized liposomal system. Further, it was converted to gel using suitable gelling agent. The optimized liposomal system and gel formulations were evaluated for various parameters. The optimized gel was evaluated for its in-vitro antifungal efficacy. The stability studies for gel were carried as per International conference on harmonisation (ICH) guidelines.&#x0D; Results: The optimized liposomal system was having vesicle size of 208.6nm, % entrapment was 91.7±1.16% and loading was 11.12±0.23%. % drug permeation was 61.10±0.85%. The zeta potential showed moderate stability. The optimized DADS liposomal gel showed satisfactory results. Ex-vivo permeation studies showed that DADS liposomal gel possesses sustained release and drug retention study proved better retention of DADS from liposomal gel than conventional gel in skin. The stability studies showed DADS liposomal gel was stable for 30 days at 25℃/60%RH, 40℃/75%RH and refrigeration (5±3℃).&#x0D; Conclusion: The results from the present study show that the sustained release profile of optimized DADS liposomal gel. The retention of DADS from liposomal gel was more than from conventional gel which helps in better pharmacological activity with least side effects.&#x0D; Keywords: Diallyl disulphide (DADS), liposomal gel, permeation, sustained release and antifungal activity.

Ex vivo transdermal absorption of a liposome formulation of diclofenac

Topical formulations of non-steroidal anti-inflammatory drugs are often used to provide effective local drug concentration while limiting systemic exposure and associated adverse events. Formulation composition has great influence on the rate of transdermal drug transport through human skin. This study was performed to compare the ex vivo transdermal transport of diclofenac from three topical formulations, a 1% liposomal gel formulation of diclofenac sodium and two emulsion gel formulations, 1.16% and 2.32% diclofenac diethylamine (equivalent to 1% and 2% diclofenac sodium). Human skin was obtained during unrelated surgical procedures and frozen at -20 °C until use. Three skin specimens were thawed, prepared for testing, and placed in a Franz cell with the stratum corneum facing the donor compartment. About 200 μl of each formulation was placed on the skin, and the receptor compartment fluid (phosphate buffered saline, pH 7.4, 32 °C) was sampled over the next 48 h. Diclofenac concentration was measured with a validated HPLC method. The transdermal permeability coefficient for the liposome 1% gel was 69.3 ± 14.4 10−8 cm•s−1, compared with 34.9 ± 9.1 10−8 cm•s−1 (P = 0.001) and 47.1±9.5 10−8 cm•s−1 (P = 0.005) for the emulsion gel 1.16% and emulsion gel 2.32%, respectively. A statistically significant difference between transdermal transport of diclofenac from the liposome gel 1% and the emulsion gel 1.16% was evident after 9 h, a clinically relevant result because these products are typically applied 2 to 4 times daily. Based on these observations, liposome gel 1% formulation of diclofenac may have a clinical advantage compared with the emulsion gel 1.16% formulation.