Recent advances in topical carriers of anti-fungal agents (original) (raw)
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Recent advances in topical formulation carriers of antifungal agents
Indian Journal of Dermatology, Venereology, and Leprology, 2015
Fungal infections are amongst the most commonly encountered diseases affecting the skin. Treatment approaches include both topical and oral antifungal agents. The topical route is generally preferred due to the possible side effects of oral medication. Advances in the field of formulation may soon render outdated conventional products such as creams, ointments and gels. Several carrier systems loaded with antifungal drugs have demonstrated promising results in the treatment of skin fungal infections. Examples of these newer carriers include micelles, lipidic systems such as solid lipid nanoparticles and nanostructured lipid carriers, microemulsions and vesicular systems such as liposomes, niosomes, transfersomes, ethosomes, and penetration enhancer vesicles.
Topical Delivery of Drugs for the Effective Treatment of Fungal Infections of Skin
Current Pharmaceutical Design, 2015
The prevalence of fungal infections of skin has increased rapidly, affecting approximately 40 million people across the globe. A wide variety of antifungal drugs has been utilized in the effective management of numerous dermatological infections. Topical treatment of fungal infections has proved to be quite advantageous due to various factors like targeting the site of infection, minimizing systemic side effects, enhanced efficacy of treatment , and improved patient compliance. In spite the fact that these agents are therapeutically active on topical application , these have restricted drug delivery across the skin resulting in insufficient therapeutic index and may exert local as well as systemic side effects. The accomplishment of topical drug delivery needs to pacify two anomalous aspects, first the barrier nature of stratum corneum, and second, deposition of drug within the skin should be ideally achieved with limited percutaneous absorption. Thus, to facilitate the delivery of antifungal drugs and improve the treatment aspects , various novel delivery carriers have been developed. This article attempts to provide an in-depth knowledge of nanoparticulate and vesicular carriers. This article focuses on the different aspects of fungal infections and their effective treatment with antifungal drugs. Efficacy of various carrier systems (nanoparticulate and vesicular carriers) in delivering antifungal drugs topically has also been discussed. Besides, compiling various research reports, this article also includes formulation considerations inclusive of regulatory aspects of ex-cipients used, the mechanisms of penetration, and patents reported.
ACTA Pharmaceutica Sciencia, 2019
Fungal infection are the common dermatological diseases. Drug delivery systems for topical use have shown significant advantages in targeting the drug to the action site in the body and also reduces the systemic side effects. In the present study an attempt was made to prepare econazole nitrate loaded nanostructured lipid carrier (NLC). Different formulations were prepared by hot homogenization technique using solid lipid and liquid lipid (GMS, GMO) and surfactants (Poloxamer 188, Poloxamer 407). Formulations were characterized for entrapment efficiency, viscosity, spreadability, pH and in vitro drug release. Entrapment efficiency of formulation F1-F8 was found to be 65.81-74.63%. The drug release of NLC gel followed zero order kinetics. NLC gel were stable at 40 ± 2ֹ°C and 75 ± 5% RH. Thus, the prepared NLC gel proved to be a potential candidate as a topical nanoparticulate sustained drug delivery system for econazole nitrate.
Nanoliposome-loaded antifungal drugs for dermal administration: A review
Current Medical Mycology, 2021
Cutaneous fungal infections are the fourth most common health problem, which involves approximately billion people worldwide. Drug delivery to the skin seems to be the best choice for superficial fungal infections. Topical formulations can release a sufficient amount of drug in therapeutical concentrations and permeate higher layers of the skin like the stratum corneum. As the outermost layer of the epidermis, the stratum corneum prevents the drug from penetrating the skin. Liposomes, especially nanosized as topical drug delivery systems to the skin, can show various functions depending on their size, lipids and cholesterol components, the percent of ingredients, lamellarity, and surface charge. Nanoliposomes can increase permeation through the stratum corneum, decrease systemic effects with their localizing actions, and overcome many dermal drug delivery obstacles. Antifungal drugs, such as croconazole, econazole, fluconazole, ketoconazole, terbinafine hydrochloride, tolnaftate, a...
Pharmaceutics
Opportunistic fungal infections are responsible for over 1.5 million deaths per year. This has created a need for highly effective antifungal medication to be as potent as possible. In this study, we improved the efficacy of a common over the counter (OTC) antifungal skin medication, miconazole, by encapsulating nano-molecules of the drug in cholesterol/sodium oleate nano-vesicles. These nano-vesicles were characterized to optimize their size, zeta potential, polydispersity index and encapsulation efficiency. Furthermore, these nano-vesicles were compared to a conventional miconazole-based commercially available cream to determine potential improvements via permeation through the stratum corneum, cytotoxicity, and antifungal capabilities. Our results found that the vesicle size was within the nano range (~300 nm), with moderate polydispersity and stability. When compared with the commercially available cream, Actavis, as well as free miconazole, the miconazole nano-vesicle formulati...
Solid Lipid Nanoparticles for Antifungal Drug Delivery System
International Journal of Engineering Applied Sciences and Technology
Fungal infections are common throughout much of the natural world. In humans, fungal infections occur when an invading fungus takes over an area of the body and is too much for the immune system to handle. Despite the availability of several effective agents in the antifungal drug, their therapeutic outcome is less than optimal due to limitations related to drug physicochemical properties and toxicity. The improvement of bioavailability of drug is the one greatest challenge in drug formulations. Many commonly used azole antifungal drugs, such as clotrimazole, miconazole, fluconazole, oxiconazole, tioconazole and sertaconazole are hydrophobic and have poor aqueous solubility. To overcome these problems, it is required to develop Lipid based nanocarrier drug delivery systems due to their capacity to increase the solubility. Hence, the purpose of this research is to formulate the wellknown antifungal agent loaded SLNs topical cream to improve its efficiency. Solid lipid nanoparticles are at the forefront of the rapidly developing field of nanotechnology with many potential applications in drug delivery, clinical medicine and research, as well as in other varied sciences. Due to their unique size-dependent properties, lipid nanoparticles offer the possibility to develop new therapeutics. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery that could be used for secondary and tertiary levels of drug targeting. Hence, solid lipid nanoparticles hold great promise for reaching the goal of controlled and site specific drug delivery and hence have attracted wide attention of researchers.
International Journal of Applied Pharmaceutics, 2024
Objective: To increase luliconazole's therapeutic impact, distribution, and preservation, this project is aimed to prepare cyclodextrin-based nanosponge gel and test its topical skin administration. Methods: The convection heating method produced cyclodextrin-diphenylcarbonate nanosponges, which later loaded with luliconazole by freezedrying. Response Surface Methodology (RSM) was used to examine the association between procedure parameters and quality variables. Pilot study findings were analyzed using Analysis of variance. Key technique factors affect quality metrics in contour, RSM, and perturbation graphs. Results: The mean medication payload was 42.19±1.45 mg of luliconazole/g of lyophilized powder. The remarkable encapsulation efficiency of luliconazole (90.12±0.92%) supports an inclusion complex. Laser light scattering evaluation of luliconazole-loaded-nanosponges shows an unimodal and narrow particle size distribution of 60-73 nm. Drug encapsulation does not change a typical nanosponge's spherical form, according to microscopic investigations. Physico-chemical characterized verified the nanosponge-luliconazole inclusion complex. The complex release is faster than pure medication in vitro. Pure luliconazole dissolves 12% in 12 h, whereas nanosponge encapsulated medicine is absorbed faster and better. After 12 h, nanosponge formulations released 93-95% luliconazole. A model carbopol gel formulation with nanosponge formulations examined skin permeability, antifungal effectiveness, and stability. In 12 h skin permeation trials, nanosponge-encapsulated luliconazole leaked slowly across rat skin. Conclusion: The slow drug release, greater skin penetration, and superior storage stability of the gel formulation based on cyclodextrin nanosponges of luliconazole imply that it has great potential as a topical delivery system.
Nanocarriers for Effective Topical Delivery of Anti-Infectives
Current Nanoscience, 2012
Skin infection is a major cause of hospital admissions as well as causes significant morbidity. Normal human skin is fortunately endowed with its own arsenal of defence strategies to preclude the ingress of pathogenic microbes. However, certain conditions compromise the barrier integrity of skin and permit pathogens to invade the skin. Skin infections may be caused by bacteria, viruses, fungi, and parasites. Topical delivery is advantageous to treat skin infections as opposed to systemic delivery owing to the direct delivery of drug to site of action, thereby reducing the doses and unwanted effects at other non-target sites. The poor penetration of anti-infective agents into skin layers makes topical therapy of skin infections formidable. Nanocarriers such as liposomes, microemulsions, and lipidic nanoparticles, have the potential to deliver drugs to the skin more efficiently than conventional topical carriers such as creams, ointments, etc. These systems have been explored by various researchers for topical delivery of antifungals, antivirals, and antibacterials. The increasing emergence of antibiotic resistant bacterial strains such as Methicillin resistant Staphylococcus aureus (MRSA) and Vancomycin resistant Enterococcus faecalis (VREF) undermine the need for new antimicrobials and new delivery systems to enhance the therapeutic efficacy of existing anti-infectives. Silver nanoparticles (SNP) have as a result made a comeback into the arsenal of antimicrobials. Also, nitric oxide (NO) releasing nanoparticles have been recently explored for their antimicrobial activity. The article showcases the immense potential of an array of nanocarriers in the treatment of cutaneous infections.
A look at emerging delivery systems for topical drug products
Dermatologic Therapy, 2011
The introduction of new topical drugs based on new chemical entities has become a rare event. Instead, pharmaceutical companies have been focused on reformulating existing drugs resulting in an ever-growing number of topical drug products for every approved drug substance. In light of this trend, soon reformulations may not be as rewarding to their sponsors as they are today unless they offer a substantial improvement over other formulations of the same drug substance and the same indication, namely improved efficacy over existing drugs, reduced side effects, unique drug combinations, or applicability for new indications. This article reviews and compares topical drug delivery systems currently under active research that are designed to offer such advantages in the coming years. The reviewed delivery systems are: liposomes, niosomes, transferosomes, ethosomes, solid lipid nanoparticles, nanostructured lipid carriers, cyclodextrin, and sol-gel microcapsules. Among all the topical drug delivery systems currently undergoing active research, only the sol-gel microencapsulation is at clinical stages.
Nanoparticles assisted intra and transdermic delivery of antifungal ointment: an updated review
Discover Nano, 2024
This review paper highlights the trans-dermic delivery of nanoparticles (NPs) based antifungal ointments with the help of nanotechnology. It also describes the novel trans-dermal approach utilizing various nanoparticles which enables an efficient delivery to the target site. This current review gives an overview about past research and developments as well as the current nanoparticle-based ointments. This review also presents data regarding types, causes of infection, and different pathogens within their infection site. It also gives information about antifungal ointments with their activity and side effects of antifungal medicines. Additionally, this review also focuses on the future aspects of the topical administration of nanoparticle-based antifungal ointments. These nanoparticles can encapsulate multiple antifungal drugs as a combination therapy targeting different aspects of fungal infection. Nanoparticles can be designed in such a way that they can specifically target fungal cells and do not affect healthy cells. Nanoparticle based antifungal ointments exhibit outstanding potential to treat fungal diseases. As further research and advancements evolve in nanotechnology, we expect more development of nanoparticle-based antifungal formulations shortly. This paper discusses all the past and future applications, recent trends, and developments in the various field and also shows its bright prospective in the upcoming years.