Novel Microemulsion Containing Benzocaine and Fusidic Acid Simultaneously: Formulation, Characterization, and In Vitro Evaluation for Wound Healing.

Modern drug carrier technologies, such as microemulsions with small droplet sizes and high surface areas, improve the ability of low water solubility active ingredients to permeate and localize. The goal of this study was to create microemulsion formulations for wound healing that contained both fusidic acid (FA), an antibacterial agent, and benzocaine (BNZ), a local anesthetic. Studies on characterization were carried out, including viscosity, droplet size, and zeta potential. The drug-loaded microemulsion had a stable structure with -3.014 ± 1.265 mV of zeta potential and 19.388 ± 0.480 nm of droplet size. In both in vitro release and ex vivo permeability studies, the microemulsion was compared with Fucidin cream and oily BNZ solution. According to the drug release studies, BNZ release from the microemulsion and the BNZ solution showed a similar profile (p > 0.05), while FA release from the microemulsion had a higher drug release compared to Fucidin cream (p < 0.001). The microemulsion presented lower drug permeation (p > 0.05) for both active ingredients, on the other hand, provided higher drug accumulation compared to the control preparations. Moreover, according to the results of in vitro wound healing activity, the microemulsion indicated a dose-dependent wound healing potential with the highest wound healing activity at the highest concentrations. To the best of our knowledge, this developed BNZ- and FA-loaded microemulsion would be a promising candidate to create new opportunities for wound healing thanks to present the active ingredients, which have low water solubility, in a single formulation and achieved higher accumulation than control preparations.

Preparation, characterization, and toxicity evaluation of microemulsion formulation containing prunetin for potential oral applications.

Phytochemicals as therapeutic alternatives can have a fundamental impact on the various stages of inflammation and its resolution. Prunetin is a naturally occurring isoflavone and has been claimed to have numerous therapeutic potentials. The objective of this study is preparation, characterization, and toxicity evaluation of microemulsion formulation containing prunetin (PMF) for potential oral applications. With this research, it was targeted to emphasize the way of improving the therapeutic efficacy of natural biomolecules with a nontoxic and effective formulation. In the study, the pseudo-ternary phase diagram was developed and PMF was characterized by conductivity, droplet size, viscosity and pH. Effects against to cytokines (IL-1ß and IL-6) and TNF-α levels of the PMF were determined by ELISA technique. Genotoxicity and acute oral toxicity tests were carried out according to OECD guidelines. The results showed that PMF is a colloid system that reduced proinflammatory cytokine levels in LPS-induced macrophage cells compared to the control group. PMF demonstrated no mutagenic activity against TA98, TA100, TA1535, and TA1537 Salmonella strains. The in vivo oral acute toxicity test results indicated that PMF did not show mortality or significant side effects even at 2000 mg/kg bw. This study represents PMF showed a good safety profile in animal study. It is thought that this formulation may have anti-inflammatory potential with further in vivo testing.

The Application of Nanogels as Efficient Drug Delivery Platforms for Dermal/Transdermal Delivery.

The delivery of active molecules via the skin seems to be an efficient technology, given the various disadvantages of oral drug administration. Skin, which is the largest human organ of the body, has the important role of acting as a barrier for pathogens and other molecules including drugs; in fact, it serves as a primary defense system blocking any particle from entering the body. Therefore, to overcome the skin barriers and poor skin permeability, researchers implement novel carriers which can effectively carry out transdermal delivery of the molecules. Another significant issue which medical society tries to solve is the effective dermal delivery of molecules especially for topical wound delivery. The application of nanogels is only one of the available approaches offering promising results for both dermal and transdermal administration routes. Nanogels are polymer-based networks in nanoscale dimensions which have been explored as potent carriers of poorly soluble drugs, genes and vaccines. The nanogels present unique physicochemical properties, i.e., high surface area, biocompatibility, etc., and, importantly, can improve solubility. In this review, authors aimed to summarize the available applications of nanogels as possible vehicles for dermal and transdermal delivery of active pharmaceutical ingredients and discuss their future in the pharmaceutical manufacturing field.

Improvement of dissolution profile of eplerenone with solidified self-emulsifying drug delivery systems (S-SEDDS).

CONTEXT: Eplerenone is a member of antihypertensives used individually or in combination with other medicines. Eplerenone exhibits poor solubility and is considered a class II drug. OBJECTIVE: Increasing the solubility of eplerenone by using both liquid and solid self-emulsifying drug delivery systems as an alternative to its marketed tablet product. METHODS: Solubility studies of eplerenone were done with different oils, surfactants, and co-surfactants to determine which one has the highest solubility for eplerenone and determine the preference in the formulations of liquid self-emulsifying drug delivery system. The solidification process was carried out with the adsorption to solid carrier method. Optimal ratios of components were specified with the pseudo-ternary phase diagram technique. Self-emulsifying drug delivery system formulations were characterized in terms of chemical interaction, droplet size/distribution, crystallization behaviors, and rheological evaluation. In vitro drug release studies were conducted and compared to pure drugs and marketed products. RESULTS: The solubility screening results showed high solubility of EPL in triacetin (11.99 mg/mL) as oil, Kolliphor®EL (≈ 2.65 mg/mL), and Tween80 (≈ 1.91 mg/mL) as surfactant and polyethylene glycol 200 (PEG200) (≈ 8.50 mg/mL), dimethyl sulfoxide (≈ 7.57 mg/mL), TranscutolP (≈ 6.03 mg/mL) as co-surfactant, respectively. Rheology studies revealed that liquid self-emulsifying drug delivery formulations exhibited non-Newtonian pseudoplastic flow. CONCLUSION: Solid self-emulsifying drug delivery systems prepared with Aerosil and Neusilin have shown tremendous improvement in terms of eplerenone dissolution by releasing the entire dose with boosted effect within 5 and 30 min respectively compared to the marketed product and pure eplerenone (p < 0.05).

Enhancing Oral Bioavailability of Domperidone Maleate: Formulation, In-Vitro Permeability Evaluation, In-Caco-2 cell Monolayers and In-Situ Rat Intestinal Permeability Studies.

BACKGROUND: The domperidone maleate, a lipophilic agent classified as a Biopharmaceutical Classification System Class II substance with weak water solubility. Self- Emulsifying Drug Delivery System is a novel approach to improve water solubility and, ultimately bioavailability of drugs. OBJECTIVE: This study aimed to develop and characterize new domperidone-loaded self-emulsifying drug delivery systems as an alternative formulation and to evaluate the permeability of domperidone-loaded self-emulsifying drug delivery systems by using Caco-2 cells and via single-pass intestinal perfusion method. METHOD: Three self-emulsifying drug delivery systems were prepared and characterized in terms of pH, viscosity, droplet size, zeta potential, polydispersity index, conductivity, etc. Each formulation underwent 10, 100, 200, and 500 times dilution in intestinal buffer pH 6.8 and stomach buffer pH 1.2, respectively. Female Sprague Dawley rats were employed for in situ single-pass intestinal perfusion investigations. RESULTS: Results of the study revealed that the ideal self-emulsifying drug delivery systems formulation showed narrow droplet size, ideal zeta potential, and no conductivity. Additionally, as compared to the control groups, the optimum formulation had better apparent permeability (12.74 ± 0.02×10-4) from Caco-2 cell monolayer permeability experiments. The study also revealed greater Peff values (2.122 ± 0.892×10-4 cm/s) for the optimal formulation from in situ intestinal perfusion analyses in comparison to control groups (Domperidone; 0.802±0.418×10-4 cm/s). CONCLUSION: To conclude, prepared formulations can be a promising way of oral administration of Biopharmaceutical Classification System Class II drugs.

Preparation and in vitro-in vivo evaluation of QbD based acemetacin loaded transdermal patch formulations for rheumatic diseases.

This research aimed to develop patches for transdermal delivery of acemetacin, which can be used to treat rheumatic diseasesand to determine their potential use. Patches were successfully created by solvent casting method using hydroxypropyl methylcellulose, propylene glycol, polyethylene glycol 400, tween 80, and dimethyl sulfoxide. Prepared patches were found using the Design of Experiments (DoE) method within the Quality by Design (QbD) approach. F1-ACM with a thickness of 0.1 ± 0.0 cm, a weight of 43.33 ± 6.29 mg, pH of 4.99 ± 0.24, moisture content of 18.33 ± 2.98%, a tensile strength of 9.196 ± 0.441 Mpa, elongation at break of 28.722 ± 0.803% and drug content of 100% was chosen as ideal formulation. 89.7% of ACM from F1-ACM was released in 5 min. F1-ACM significantly (p < 0.05) increased the response latency to the thermal stimulus at 90th (3.071 ± 0.517) and 120th (3.87 ± 0.332) min in the hot plate test. In the tail-flick experiment, F1-ACM significantly (p < 0.05) increased the reaction delay against heat stimuli at 90th (3.016 ± 0.695), 120th (2.884 ± 0.851), and 180th (2.893 ± 0.932) min. F1-ACM patch significantly (p < 0.001) inhibited paw edema formation at 1, 2, 3, 4, and 5 h after induction of inflammation as compared to the control group. Therefore, this formulation can be employed more efficiently for rheumatic disease.

Protein and Gene Delivery Systems for Neurodegenerative Disorders: Where Do We Stand Today?

It has been estimated that every year, millions of people are affected by neurodegenerative disorders, which complicate their lives and their caregivers' lives. To date, there has not been an approved pharmacological approach to provide the complete treatment of neurodegenerative disorders. The only available drugs may only relieve the symptoms or slow down the progression of the disease. The absence of any treatment is quite rational given that neurodegeneration occurs by the progressive loss of the function or structure of the nerve cells of the brain or the peripheral nervous system, which eventually leads to their death either by apoptosis or necrotic cell death. According to a recent study, even though adult brain cells are injured, they can revert to an embryonic state, which may help to restore their function. These interesting findings might open a new path for the development of more efficient therapeutic strategies to combat devastating neurodegenerative disorders. Gene and protein therapies have emerged as a rapidly growing field for various disorders, especially neurodegenerative diseases. Despite these promising therapies, the complete treatment of neurodegenerative disorders has not yet been achieved. Therefore, the aim of this review is to address the most up-to-date data for neurodegenerative diseases, but most importantly, to summarize the available delivery systems incorporating proteins, peptides, and genes that can potentially target such diseases and pass into the blood-brain barrier. The authors highlight the advancements, at present, on delivery based on the carrier, i.e., lipid, polymeric, and inorganic, as well as the recent studies on radiopharmaceutical theranostics.

Azelaic acid loaded chitosan and HPMC based hydrogels for treatment of acne: formulation, characterization, in vitro-ex vivo evaluation.

In this study, hydrogels containing azelaic acid were developed using chitosan or HPMC (1-7%) for local treatment of acne vulgaris. Physicochemical properties such as viscosity, pH and mechanical properties were evaluated. In vitro release and ex vivo permeability studies were performed using the Franz diffusion cell system. The pH of the hydrogels was highly compatible with the skin pH and varied between 4.38 and 5.84. The cumulative release percentages of the hydrogels at the end of 6 hours were 65-78%, whereas the marketed product yielded 50% drug release. According to the ex vivo permeability results, azelaic acid accumulated in the skin was found to be 9.38 ± 0.65% (marketed cream), 19.53 ± 1.06% (K3), 10.96 ± 1.91% (H6). The antiacne studies with Cutibacterium acnes revealed that K3 (29.45 ± 0.95) and H6 (32.35 ± 0.15) had higher inhibition zones compared to the marketed cream (24.50 ± 0.90). Additionally, the gels were found to be highly stable as a result of the stability studies for 6 months. Among the hydrogels that were prepared based on experimental findings, K3 (3% Chitosan) and H6 (6% HPMC) represented elevated in vitro release profile, higher permeability and increased antiacne activity. The findings of this research suggest that the developed hydrogels might be an alternative to the marketed product.

New topical microemulsions of etofenamate as sufficient management of osteoarthritis

Abstract In this study, microemulsions containing etofenamate were prepared and evaluated as dermal delivery carriers. The developed microemulsions consist of oleic acid, Span 80, Tween 20, Cremophor EL, Transcutol and ethanol. The percentage of etofenamate loading in the microemulsions was 5% (w/w). The characterization of formulations included droplet size, zeta potential, pH, conductivity, PDI, refractive index and viscosity. Moreover, ex vivo penetration study was carried out using mice abdominal skin. The developed formulations were analyzed for their cytotoxicity via MTT assay and tested for their anti-inflammatory properties opposed to LPS-stimulated nitrite prοduction in RAW 264.7 cells. As ideal formulation, M2ETF, was chosen due to its greater permeation, lower penetration as well as higher anti-inflammatory

Chitosan-bovine serum albumin-Carbopol 940 nanogels for mupirocin dermal delivery: ex-vivo permeation and evaluation of cellular binding capacity via radiolabeling.

The goal of this study was to develop and examine the nanogel-based topical delivery system of mupirocin. Nanogels were prepared with chitosan and bovine serum albumin by ionic gelation and Carbopol 940 was added to improve the gelling/adhesive properties. Detailed characterization studies were performed and the cellular binding capacity of radiolabeled nanogels was investigated on CCD-1070Sk cell lines. Results indicate the successful formation of nanogels with particle size and zeta potential ranged between 341.920-603.320 nm and 13.120-24.300 mV, respectively. The mechanical and rheological studies proved pseudoplastic and strong elastic gel behavior (G' > G''). Mupirocin was successfully entrapped into nanogels with a ratio of more than 95% and the loaded drug was slowly released up to 93.89 ± 3.07% within 24 h. The ex vivo penetration and permeation percentages of mupirocin were very low (1.172 ± 0.202% and 0.161 ± 0.136%) indicating the suitability of nanogels for dermal use against superficial skin infections. The microbiological studies pointed out the effectiveness of nanogels against Staphylococcus aureus strains. Nanogels did not show toxicity signs and the cell binding capacity of radiolabeled formulations was found to be higher than [99mTc]NaTcO4 to CCD-1070Sk cell line. Overall, mupirocin nanogels might be considered as a potential and safe topical treatment option for bacterial skin infections.

Current Status of Pediatric Formulations for Chronic and Acute Children' Diseases: Applications and Future Perspectives.

Infants and other children can be affected by various acute, chronic and many of them rare illnesses. Developing drugs for children is very challenging since they cannot intake tablets or hard oral solid dosage forms. Besides, most of the prescribed pediatric medications are unlicensed. The biggest issue that clinicians have to solve is that dosing in children is not based on weight or surface area of the body, as it happened in adults but is related to age variations in drug absorption, distribution, metabolism, and elimination. Thus, for pediatric patients, various therapeutic approaches have been proposed so as to develop suitable formulations such as liquid dosage forms, flexible capsules, milk-based products, etc. In addition, the administration of current pharmaceutical products to children might lead to some serious side effects which can also happen in adults but with a lower risk. Especially, infants are at high risk of getting poisoned by taking drugs used for adults. Moreover, children are very sensitive to the taste and smell of some pharmaceutical vehicles and can resist to intake them and this situation leads parents to search for tasteless and odorless medications. In this study, the current formulations for various diseases intended to be used in pediatric patients as well as various chronic and acute diseases of childhood are summarized. Authors believe that this review can help professionals who want to work with pediatric formulations to design more efficient and child-friendly drug delivery systems.

Ocular microemulsion of brinzolamide: Formulation, physicochemical characterization, and in vitro irritation studies based on EpiOcular™ eye irritation assay.

In recent years, the hydrophobic active substances have led researchers to develop new formulations to enhance bioavailability and dissolution rate; brinzolamide, a lipophilic drug belongs to carbonic anhydrase inhibitors, which cause reduction of intraocular pressure in patients suffering from glaucoma. Currently, the marketed product of brinzolamide is in the form of ocular drops; nonetheless, the conventional drops provide decreased therapeutic efficacy owing to their low bioavailability and pulsed drug release. Thus, the development of novel ocular formulations such as topical microemulsions is of high importance. In this work, the preparation of new microemulsions containing brinzolamide (0.2, 0.5 and 1% w/w) and comprised from isopropyl myristate, tween 80 and span 20 and Cremophor EL was performed. The obtained microemulsions were further characterized for their physicochemical properties. In addition, Fourier Transformed-Infrared spectroscopy was used touate the compatibility of active ingredients and components. In vitro release studies along with kinetic modeling were performed using the dialysis membrane method in simulated tear fluid. Bioadhesion studies were performed using Texture analysis. Finally, in vitro ocular irritation based on EpiOcular™ Eye Irritation Test and cytocompatibility studies was performed to examine any possible harm on ocular cells and predict in vivo safety profile.

Promising nanogels loaded with usnic acid for oral ulcer treatment: development, characterization, and in vivo evaluation in rabbits.

This study aimed to present an effective formulation targeting oral ulcers that will remain in the application site for a longer period, reducing the frequency of administration. As a candidate formulation, usnic acid (UA) was loaded into the optimum nanogels. The characterization studies included physical, rheological, and bioadhesive properties as well as in vitro release and ex vivo studies. The rheological results revealed that the nanogels present pseudoplastic flow behavior. In vitro drug release showed a prolonged pattern. In further, the chosen UA nanogels showed very low percentages of penetration and permeation. F13, which showed the highest release, suitable bioadhesive properties (0.475 ± 0.033 N/cm2) and eligible particle size (250.22 ± 4.11 nm), PDI (0.089 ± 0.052), and zeta potential (20.56 ± 0.330 mV) values were chosen for in vivo experiments. The selected UA nanogels showed effective antimicrobial activity against Bacillus Cereus and great in vivo wound healing properties. The results indicated that suitable UA nanogels with desired properties could be prepared. The therapeutic potential of the nanogels for oral ulcers was assessed using an animal model and the histopathological findings suggested that the optimized formulation is a good choice for oral ulcer treatment. Nonetheless, further research is recommended to support its efficacy by applying pharmacodynamic and pharmacokinetic studies in human individuals.

Detecting and targeting neurodegenerative disorders using electrospun nanofibrous matrices: current status and applications.

Neurodegeneration is defined as the progressive atrophy and loss of function of neurons; it is present in neurodegenerative disorders such as Multiple Sclerosis, Alzheimer's, Huntington's, and Parkinson's diseases. The detection of such disorders is performed by various imaging modalities while their therapeutic management is quite challenging. Besides, the pathogenesis of neurodegenerative disorders is still under ongoing research due to complex and multi-factorial mechanisms. Currently, targeting the specific proteins responsible for neurodegeneration is of great interest to many researchers. Furthermore, nanotechnology-based approaches for targeting the affected neurons became an emerging field of interest. Nanostructures of various forms have been developed aiming to act as therapeutics for neurodegeneration, in which electrospun nanofibers seem to play an important role as biomedical products for both detection and management of the diseases. Electrospinning is an intriguing method able to produce nanofibers with a wide range of sizes and morphological characteristics. Such nanofibrous matrices can be delivered through different administration routes to target various diseases. In this review, the most recent advancements in electrospun nanofibrous systems that target or detect multiple neurodegenerative diseases have been enlightened and an introduction to the general aspects of neurodegenerative diseases and the electrospinning process has been made. Finally, future perspectives of neurodegeneration targeting were also discussed.

Recent trends on wound management: New therapeutic choices based on polymeric carriers.

Wound healing is an unmet therapeutic challenge among medical society since wound assessment and management is a complex procedure including several factors playing major role in healing process. Wounds can mainly be categorized as acute or chronic. It is well referred that the acute wound displays normal wound physiology while healing, in most cases, is seemed to progress through the normal phases of wound healing. On the other hand, a chronic wound is physiologically impaired. The main problem in wound management is that the majority of wounds are colonized with microbes, whereas this does not mean that all wounds will be infected. In this review, we address the problems that clinicians face to manage while treat acute and chronic wounds. Moreover, we demonstrate the pathophysiology, etiology, prognosis and microbiology of wounds. We further introduce the state of art in pharmaceutical technology field as part of wound management aiming to assist health professionals to overcome the current implications on wound assessment. In addition, authors review researches which included the use of gels and dermal films as wound healing agents. It can be said that natural and synthetic drugs or carriers provide promising solutions in order to meet the wound management standards. However, are the current strategies as desirable as medical society wish?

New therapeutic system based on hydrogels for vaginal candidiasis management: formulation-characterization and in vitro evaluation based on vaginal irritation and direct contact test.

The objective of the present research was to examine the possible usage of terbinafine loaded hydrogels for vaginal application as part of vaginal candidiasis treatment. Vaginal candidiasis belongs to the most frequent gynecological disorders. Various antifungal drugs are used for its treatment, with Terbinafine being one of them. In this study, new gel formulations were prepared for Terbinafine vaginal delivery. Natural polymers such as chitosan, sodium carboxymethylcellulose, and Carbopol were used for the development of Terbinafine vaginal gels. The developed gels were examined for their viscosity and spreadability, pH and mechanical properties. The most optimal formulations were further evaluated for their in vitro release behavior and antifungal activities. In further, the cytotoxicity and irritation inducing capacity of optimum gel formulations were evaluated. In vitro drug release studies demonstrated that terbinafine release was prolonged whereas anti-candida activity in several species showed the superiority of the gels compared to the marketed product. G-5 and G-8 gels did not cause lysis, hemorrhage and coagulation, therefore, classified as non-irritant. The optimal formulations were also studied for their stability, demonstrating that they were stable for 3 months.

In Vivo Wound Healing and In Vitro Anti-Inflammatory Activity Evaluation of Phlomis russeliana Extract Gel Formulations.

The air-dried aerial parts of Phlomis russeliana (Sims) Lag. Ex Benth. was extracted by methanol and fractionated by n-hexane, dichloromethane, and ethyl acetate, respectively. The wound healing properties of P. russeliana extract gel was evaluated using the in vivo excisional wound model using Balb-c mice. Initially, the P. russeliana methanol extract showed LOX inhibitory activity at IC50 = 23.2 µg/mL, whereas the DPPH• assay showed IC50 = 0.89 mg/mL, and the ABTS• assay showed IC50 = 0.99 mg/mL, respectively. In addition, a remarkable anti-inflammatory activity was observed in the cell culture assay. Thereafter, activity-guided fractionation was performed by LOX enzyme inhibition assays, and the structures of the two most active fractions were revealed by both GC-FID and GC/MS analyses, simultaneously. Phytol and 1-heptadecanoic acid were characterized as the active constituents. Moreover, the P. russeliana extract gel formulation was applied for in vivo tests, where the new gel formulation supported the in vitro anti-inflammatory activity findings. As a conclusion, this experimental results support the wound healing evidence based on the ethnobotanical application of Phlomis species with further potential.

Tazarotene-loaded in situ gels for potential management of psoriasis: biocompatibility, anti-inflammatory and analgesic effect.

Psoriasis is a chronic autoinflammatory disorder characterized by patches of abnormal skin. For psoriasis management, the application of topical retinoids as Tazarotene is recommended. However, Tazarotene could induce skin irritation limiting its use. Herein, it is evaluated the possible usage of in situ gels for tazarotene skin delivery. The topical in situ gels were developed using thermosensitive poloxamers via cold method. They were examined for their appearance, sol-gel temperature, clarity, pH, viscosity, in vitro release, and stability. Their biocompatibility was evaluated by investigating their cytotoxicity and irritation inducing capacity. The possible anti-inflammatory and analgesic activities were determined by measuring the nitric oxide and prostaglandin E2 levels production in LPS-stimulated RAW264.7 murine macrophage cells. It was revealed that the in situ gels had no cytotoxic effect (∼95-100% cell viability) and nor irritation potential (∼97% cell viability), according to the in vitro EpiDerm™ reconstituted skin irritation test. Additionally, the 10% tazarotene-in situ gels showed possible analgesic activity since the production of prostaglandin E2 (PGE2) was decreased. In further, both concentrations of 5% and 10% tazarotene-in situ gels inhibited significantly the nitrite oxide production at 16% and 19%, respectively. Finally, the prepared in situ gels can act as a potential non-irritant alternative option for tazarotene topical skin delivery.

Novel Ocular Drug Delivery Systems: An Update on Microemulsions.

Sufficient ophthalmic drug delivery is still challenging for pharmaceutical technologists, despite various scientific efforts. Several ocular drug carriers have been designed to enhance bioavailability by prolonging the drug retention time. One of the current encouraging approaches is the utilization of colloidal carriers with the characteristic submicron-nanometer size. Microemulsions (MEs) are such colloid systems that present sizes between 5 and 200 nm with significant thermodynamic stability and low surface tension. In addition, MEs as topical ocular carriers can lead to great ocular drug adsorption due to their enhanced retention time. Furthermore, considering that MEs are stable for long time and various temperatures, their ocular application is of great interest. The aim of this study is to cover basic physicochemical principals of ocular MEs such as their possible size, stability, and therapeutic efficacy against various eye disorders. Thus, a comprehensive review for ocular drug delivery systems in the form of MEs that show promising characteristics as their stability and therapeutic efficiency is performed.

Evaluation of burn wound healing activity of novel fusidic acid loaded microemulsion based gel in male Wistar albino rats.

The objective of the present research was to examine the possible usage of microemulsion based gel for fusidic acid (FA) dermal application as burn wound treatment. During the preparation of microemulsion, ethyl oleate as oil phase, tween 80 as a surfactant, ethanol as co-surfactant, water as aqueous phase were used. The prepared microemulsions were evaluated for clarity, pH, viscosity and FA content. Moreover, stability, sterility, antibacterial activity, in vitro release of the formulations were also evaluated. The results showed that the FA loaded microemulsion and microemulsion based gel formation and characteristics were related to many parameters of the components. The performed optimized microemulsion-based gel showed good stability over a period of 3 months. The antibacterial activity of microemulsion-based gel was found to be comparable with marketed cream. RAW 264.7 macrophages were used to determine cell viability (MTT assay) and nitric oxide production. MBG and FA-MBG significantly inhibit the production of the inflammatory mediator NO in LPS-stimulated RAW 264.7 cells in a concentration-dependent manner. The wound healing property was evaluated by histopathological examination and by measuring the wound contraction. The % of wound area in rats treated with FA (2%) loaded microemulsion based gel ranged from 69.30% to 41.39% in the period from 3 to 10 days. In conclusion, FA loaded microemulsion based gel could be offered as encouraging strategy as dermal systems for the burn wound treatment.