Topical Drug Delivery of Anti-infectives Employing Lipid-Based Nanocarriers: Dermatokinetics as an Important Tool

2019 ◽  
Vol 24 (43) ◽  
pp. 5108-5128 ◽  
Author(s):  
Kanika Thakur ◽  
Gajanand Sharma ◽  
Bhupindar Singh ◽  
Om Prakash Katare
Keyword(s):  
Drug Delivery ◽  
Infectious Diseases ◽  
Patient Compliance ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Controlled Drug Release ◽  
Topical Drug Delivery ◽  
Promising Strategy ◽  
Drug Resistant Strains

Background:The therapeutic approaches for the management of topical infections have always been a difficult approach due to lack of efficacy of conventional topical formulations, high frequency of topical applications and non-patient compliance. The major challenge in the management of topical infections lies in antibiotic resistance which leads to severe complications and hospitalizations resulting in economic burden and high mortality rates.Methods:Topical delivery employing lipid-based carriers has been a promising strategy to overcome the challenges of poor skin permeation and retention along with large doses which need to be administered systemically. The use of lipid-based delivery systems is a promising strategy for the effective topical delivery of antibiotics and overcoming drug-resistant strains in the skin. The major systems include transfersomes, niosomes, ethosomes, solid lipid nanoparticles, nanostructured lipid carriers, microemulsion and nanoemulsion as the most promising drug delivery approaches to treat infectious disorders. The main advantages of these systems include lipid bilayer structure which mimics the cell membrane and can fuse with infectious microbes. The numerous advantages associated with nanocarriers like enhanced efficacy, improvement in bioavailability, controlled drug release and ability to target the desired infectious pathogen have made these carriers successful.Conclusion:Despite the number of strides taken in the field of topical drug delivery in infectious diseases, it still requires extensive research efforts to have a better perspective of the factors that influence drug permeation along with the mechanism of action with regard to skin penetration and deposition. The final objective of the therapy is to provide a safe and effective therapeutic approach for the management of infectious diseases affecting topical sites leading to enhanced therapeutic efficacy and patient-compliance.

Development and Evaluation of Ketoconazole Loaded Nano-sponges for Topical Drug Delivery

2018 ◽  
Vol 11 (4) ◽  
pp. 4154-4162
Author(s):  
Harshal A. Pardeshi ◽  
Makarand S Gambhire ◽  
Kishore N. Gujar ◽  
Aniket A Vaidhya
Keyword(s):  
Drug Delivery ◽  
Antifungal Activity ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Controlled Drug Release ◽  
Topical Drug Delivery ◽  
Molar Ratios ◽  
Skin Targeting ◽  
Skin Retention

Beta-cyclodextrin nanosponges (NS) based hydrogel had been studied as a topical delivery of ketoconazole (KTZ) for effective eradication of cutaneous fungal infection. The purpose of the present study was to develop KTZ loaded NS for topical drug delivery with skin targeting to minimizing the adverse side effects and providing a controlled release. The four types of NS were synthesized by varying the molar ratios of β-cyclodextrin (β-CD) to diphenylcarbonate (DPC) as a cross linker viz. 1:2, 1:4, 1:6, and 1:8. The KTZ loaded NS shows particle size 274.6-367 nm and high loading efficacy was obtained, FTIR, DSC, XRD studies confirmed the complexation of KTZ with NS. Hydrogel were evaluated comparatively with commercial product with respect to physicochemical properties, ex-vivo skin permeation and skin retention on human cadaver skin and antifungal activity. Ex-vivo study of KTZ-NS hydrogel exhibited controlled drug release up to 8 hrs whereas skin retention studies show avoidance of the systemic uptake and better accumulative uptake of the drug compared to marketed formulation. The zone of inhibition of KTZ-NS hydrogel was higher in comparison with commercial formulation against Candida albicans. These results indicate that the KTZ-NS is having controlled drug release, potential of skin targeting with enhanced antifungal activity.

The factors determining the skin penetration and cellular uptake of nanocarriers: New hope for clinical development

2021 ◽  
Vol 27 ◽  
Author(s):  
Afsaneh Farjami ◽  
Sara Salatin ◽  
Samira Jafari ◽  
Mohammad Mahmoudian ◽  
Mitra Jelvehgari
Keyword(s):  
Drug Delivery ◽  
Skin Permeation ◽  
Direct Interaction ◽  
Skin Barrier ◽  
Skin Penetration ◽  
Physicochemical Characteristics ◽  
Skin Permeability ◽  
Topical Drug Delivery ◽  
Major Barrier ◽  
Composition And Structure

: The skin provides a protective barrier against toxic environments and also offers a valuable route for topical drug delivery. The stratum corneum (SC) is the outermost layer of the skin and serves as the major barrier to chemical transfer through the skin. The human skin barrier is particularly diffcult to overcome because of the complex composition and structure of the SC. Nanoparticulate carriers have gained widespread attention in topical drug delivery due to their tunable and versatile properties. The present review summarizes the main factors involved in the skin penetration of nanocarriers containing drug. Employment of nanotechnology in topical delivery has grown progressively during recent years; however, it is important to monitor the skin penetration of nanocarriers prior to their use due to avoid possible toxic effects. Nanocarriers can act as a means to increase the skin permeation of drugs by supporting a direct interaction with the SC and increasing the period of permanence on the skin. The skin penetration is influenced by the physicochemical characteristics of nanocarriers such as composition, size, shape, surface chemistry as well as skin features. Considering that the target of topical systems based on nanocarriers is the penetration of therapeutic agents in the skin layers, so a detailed understanding of the factors influencing skin permeability of nanocarriers is essential for safe and efficient therapeutic applications.

Nanotechnological Innovations Enhancing the Topical Therapeutic Efficacy of Quercetin: A Succinct Review

2020 ◽  
Vol 17 (4) ◽  
pp. 270-278
Author(s):  
Maha Nasr ◽  
Rawan Al-Karaki
Keyword(s):  
Side Effects ◽  
Therapeutic Efficacy ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Natural Compounds ◽  
Therapeutic Activity ◽  
Dermatological Diseases ◽  
Anti Inflammatory ◽  
Topical Applications

Nanotechnology is currently a hot topic in dermatology and nutraceutical/cosmeceutical delivery, owing to the advantages it provides in terms of enhancing the skin permeation of drugs, as well as increasing their therapeutic efficacy in the treatment of different dermatological diseases. There is also a great interest in the topical delivery of nutraceuticals; which are natural compounds with both therapeutic and cosmetic benefits, in order to overcome the side effects of topically applied chemical drugs. Quercetin is a key nutraceutical with topical antioxidant and anti-inflammatory properties which was reported to be effective in the treatment of different dermatological diseases, however, its topical therapeutic activity is hindered by its poor skin penetration. This review highlights the topical applications of quercetin, and summarizes the nanocarrier-based solutions to its percutaneous delivery challenges.

scholarly journals FORMULATION AND IN VITRO CHARACTERISATION OF SOYBEAN OIL-HPMCK4M BASED BIGEL MATRIX FOR TOPICAL DRUG DELIVERY

2019 ◽  
pp. 33-38
Author(s):  
SHUBHAM MUKHERJEE ◽  
SUTAPA BISWAS MAJEE ◽  
GOPA ROY BISWAS
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Soybean Oil ◽  
Skin Permeation ◽  
Topical Drug Delivery ◽  
Zero Order Kinetics ◽  
Wide Range ◽  
Span 60 ◽  
Hydrophilic Gel

Objective: Hydrogels with scope for utilization in numerous fields possess limited applications due to problems in incorporating wide range of drugs and crossing the lipophilic barrier of the skin. Attempts to overcome these problems by developing organogel hold drawbacks. Challenges posed by drug lipophilicity or skin permeation can be solved by developing bigel formed via combination of lipophilic and hydrophilic gel phases in a definite proportion. The objective of the present study is to formulate and characterize matrix type bigel of soybean oil and HPMCK4M for topical drug delivery. Methods: Four batches of bigels were developed with two organogel formulations of soybean oil containing 20 and 22% w/v Span 60. Both organogels and bigels were examined for compatibility by FTIR spectroscopy, hemocompatibility and characterized for physical appearance, pH, rheological behavior and in vitro drug release pattern. Results: FTIR study confirmed compatibility between paracetamol and components of organogel or bigel. The oily feel of organogels disappeared with bigels which possessed a creamy and smooth texture. Pseudoplastic behaviour was confirmed by Ostwald-de wale power-law model in both organogels and bigels. Improved drug release was observed in bigel (BG1) formulation containing 3%w/v HPMCK4M and soybean oil based organogel with 20% w/v Span 60 as compared to the corresponding organogel (OG1). Organogels were foundto follow either zero-order kinetics (OG1) or Korsmeyer-Peppasmodel (OG2) while the formation of matrix was exhibited in bigels with drug diffusion predominantly of non-Fickian type. Conclusion: Therefore, bigels of soybean oil based organogel with HPMCK4M hydrogel formed gel matrix demonstrating improved drug release for topical application compared to organogel.

scholarly journals Nanotechnology-Based Topical Drug Delivery Systems for Management of Dandruff and Seborrheic Dermatitis: An overview

2020 ◽  
Vol 29 (1) ◽  
pp. 12-32
Author(s):  
Lena M. Thomas ◽  
Abeer H. Khasraghi
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Therapeutic Efficacy ◽  
Drug Delivery Systems ◽  
Seborrheic Dermatitis ◽  
Delivery Systems ◽  
Drug Formulation ◽  
Topical Drug Delivery ◽  
Skin Disorders ◽  
Common Skin

Dandruff and seborrheic dermatitis (SD) are common skin disorders affecting the scalp and extending to other body sites in the case of SD. They are associated with pruritus and scaling, causing an esthetical disturbance in the population affected.   Treatment of such conditions involves using a variety of drugs for long terms, thus optimizing drug formulation is essential to improve therapeutic efficacy and patient compliance. Conventional topical formulations like shampoos and creams have been widely used but their use is associated with disadvantages. To overcome such effects, novel topical nanotechnology-based formulations are currently under investigation. In the following article, we highlight recently published formulation approaches used to improve topical dandruff/SD therapy

Ionic liquids with N-methyl-2-pyrrolidonium cation as an enhancer for topical drug delivery: Synthesis, characterization, and skin-penetration evaluation

2020 ◽  
Vol 299 ◽  
pp. 112166 ◽  
Author(s):  
Rahman Md Moshikur ◽  
Md Raihan Chowdhury ◽  
Rie Wakabayashi ◽  
Yoshiro Tahara ◽  
Noriho Kamiya ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Ionic Liquids ◽  
Skin Penetration ◽  
Topical Drug Delivery

Limitations and Opportunities in Topical Drug Delivery: Interaction Between Silica Nanoparticles and Skin Barrier

2019 ◽  
Vol 25 (4) ◽  
pp. 455-466 ◽  
Author(s):  
Francisco Arriagada ◽  
Javier Morales
Keyword(s):  
Drug Delivery ◽  
Adverse Effects ◽  
Silica Nanoparticles ◽  
Skin Barrier ◽  
Skin Penetration ◽  
Bioactive Compound ◽  
Penetration Enhancers ◽  
Topical Drug Delivery ◽  
Skin Delivery ◽  
The Stability

The first limiting barrier for the transport in the skin is the stratum corneum; different strategies have been developed to overcome this barrier, including chemical enhancers. However, these penetration enhancers have limitations, including toxic adverse effects. In this context, research into nanomaterials has provided new tools to increase the residence time of drugs by generating a reservoir, increasing the specificity of drugs and reducing their adverse effects, and improving the penetration of drugs that are difficult to formulate. Silica nanoparticles have been proposed as suitable nanocarriers for skin delivery. Unfortunately, the mechanisms involved in the interaction, transport and fate of silica nanoparticles in the skin have not been fully investigated. This paper reviews significant findings about the interaction between silica-based nanocarriers and the skin. First, this review focuses on the properties and functions of the skin, the skin penetration properties of silica nanoparticles, their synthesis strategies and their toxicity. Finally, advances and evidence on the application of silica nanocarriers in skin drug delivery are provided, in which the use of nanoparticles increases the stability and solubility of the bioactive compound, enhancing its performance, act as penetrator enhancer and improving controlled release. Thus, improving the treatment of some skin disorders.

Transfersomes as alternative topical nanodosage forms for the treatment of skin disorders

Nanomedicine ◽  
2021 ◽  
Author(s):  
Pablo Oyarzún ◽  
Eduardo Gallardo-Toledo ◽  
Javier Morales ◽  
Francisco Arriagada
Keyword(s):  
Drug Delivery ◽  
Topical Treatment ◽  
Skin Penetration ◽  
Unique Characteristic ◽  
Topical Drug Delivery ◽  
Skin Disorders ◽  
Therapeutic Applications ◽  
Clinical Benefits ◽  
Pass Through

Topical drug delivery is a promising approach to treat different skin disorders. However, it remains a challenge mainly due to the nature and rigidity of the nanosystems, which limit deep skin penetration, and the unsuccessful demonstration of clinical benefits; greater penetration by itself, does not ensure pharmacological success. In this context, transfersomes have appeared as promising nanosystems; deformability, their unique characteristic, allows them to pass through the epidermal microenvironment, improving the skin drug delivery. This review focuses on the comparison of transfersomes with other nanosystems (e.g., liposomes), discusses recent therapeutic applications for the topical treatment of different skin disorders and highlights the need for further studies to demonstrate significant clinical benefits of transfersomes compared with conventional therapies.

scholarly journals Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

2021 ◽  
Vol 22 (4) ◽  
pp. 1535
Author(s):  
Parinbhai Shah ◽  
Benjamin Goodyear ◽  
Nirali Dholaria ◽  
Vinam Puri ◽  
Bozena Michniak-Kohn
Keyword(s):  
Drug Delivery ◽  
Skin Diseases ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Oral Drug ◽  
Ionic Surfactant ◽  
Content Uniformity ◽  
Drug Bioavailability ◽  
Drug Content

Psoriasis is a chronic autoimmune skin disease impacting the population globally. Pharmaceutical products developed to combat this condition commonly used in clinical settings are IV bolus or oral drug delivery routes. There are some major challenges for effectively developing new dosage forms for topical use: API physicochemical nature, the severity of the disease state, and low bioavailability present challenges for pharmaceutical product developers. For non-severe cases of psoriasis, topical drug delivery systems may be preferred or used in conjunction with oral or parenteral therapy to address local symptoms. Elastic vesicular systems, termed “niosomes”, are promising drug delivery vehicles developed to achieve improved drug delivery into biological membranes. This study aimed to effectively incorporate a corticosteroid into the niosomes for improving the drug bioavailability of desoximetasone, used to treat skin conditions via topical delivery. Niosomes characterization measurements were drug content, pH, spreadability, specific gravity, content uniformity, rheology, and physicochemical properties. Formulations used a topical gelling agent, Carbomer 980 to test for in vitro skin permeation testing (IVPT) and accelerated stability studies. The developed niosomal test gel provided approximately 93.03 ± 0.23% to 101.84 ± 0.11% drug content with yield stresses ranging from 16.12 to 225.54 Pa. The permeated amount of desoximetasone from the niosomal gel after 24 h was 9.75 ± 0.44 µg/cm2 compared to 24.22 ± 4.29 µg/cm2 released from the reference gel tested. Furthermore, a drug retention study compared the test gel to a reference gel, demonstrating that the skin retained 30.88 ng/mg of desoximetasone while the reference product retained 26.01 ng/mg. A controlled drug release profile was obtained with a niosomal formulation containing desoximetasone for use in a topical gel formulation showing promise for potential use to treat skin diseases like psoriasis.

scholarly journals Non-Invasive Topical Drug-Delivery System Using Hyaluronate Nanogels Crosslinked via Click Chemistry

Materials ◽  
2021 ◽  
Vol 14 (6) ◽  
pp. 1504
Author(s):  
Hyunsik Choi ◽  
Mina Kwon ◽  
Hye Eun Choi ◽  
Sei Kwang Hahn ◽  
Ki Su Kim
Keyword(s):  
Drug Delivery ◽  
Click Chemistry ◽  
Topical Delivery ◽  
Topical Drug Delivery ◽  
Safety Issues ◽  
Non Invasive ◽  
Therapeutic Drugs ◽  
Delivery Routes ◽  
Model Drug

Hyaluronate (HA) has been widely investigated for noninvasive topical drug delivery of chemical drugs and biopharmaceuticals. However, previous noninvasive delivery systems have been facilitated mostly by chemical conjugation of drugs with HA, which can cause reduced therapeutic efficacy and safety issues in chemically modified drugs. Here, HA nanogels were synthesized by crosslinking via “click” chemistry for noninvasive topical delivery of a model drug without chemical modification. The model-drug-encapsulating HA nanogels could be uptaken to the skin melanoma cells in vitro by HA-mediated endocytosis. In addition, histological analysis showed that HA nanogels could be topically delivered to the deep skin and tongue tissues through the noninvasive delivery routes. Taken together, HA nanogels could be effectively used for the noninvasive topical delivery of various therapeutic drugs.

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