scholarly journals Topical Administration of Drugs Incorporated in Carriers Containing Phospholipid Soft Vesicles for the Treatment of Skin Medical Conditions

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2129
Author(s):  
Elka Touitou ◽  
Hiba Natsheh

This review focuses on the improved topical treatment of various medical skin conditions by the use of drugs delivered from carriers containing phospholipid soft vesicles. Topical drug delivery has many advantages over other ways of administration, having increased patient compliance, avoiding the first-pass effect following oral drug administration or not requesting multiple doses administration. However, the skin barrier prevents the access of the applied drug, affecting its therapeutic activity. Carriers containing phospholipid soft vesicles are a new approach to enhance drug delivery into the skin and to improve the treatment outcome. These vesicles contain molecules that have the property to fluidize the phospholipid bilayers generating the soft vesicle and allowing it to penetrate into the deep skin layers. Ethosomes, glycerosomes and transethosomes are soft vesicles containing ethanol, glycerol or a mixture of ethanol and a surfactant, respectively. We review a large number of publications on the research carried out in vitro, in vivo in animal models and in humans in clinical studies, with compositions containing various active molecules for treatment of skin medical conditions including skin infections, skin inflammation, psoriasis, skin cancer, acne vulgaris, hair loss, psoriasis and skin aging.

2021 ◽  
Vol 9 (7) ◽  
pp. 1486
Author(s):  
Marcela Espinoza-Monje ◽  
Jorge Campos ◽  
Eduardo Alvarez Villamil ◽  
Alonso Jerez ◽  
Stefania Dentice Maidana ◽  
...  

Previously, we isolated lactic acid bacteria from the slime of the garden snail Helix aspersa Müller and selected Weissella viridescens UCO-SMC3 because of its ability to inhibit in vitro the growth of the skin-associated pathogen Cutibacterium acnes. The present study aimed to characterize the antimicrobial and immunomodulatory properties of W. viridescens UCO-SMC3 and to demonstrate its beneficial effect in the treatment of acne vulgaris. Our in vitro studies showed that the UCO-SMC3 strain resists adverse gastrointestinal conditions, inhibits the growth of clinical isolates of C. acnes, and reduces the adhesion of the pathogen to keratinocytes. Furthermore, in vivo studies in a mice model of C. acnes infection demonstrated that W. viridescens UCO-SMC3 beneficially modulates the immune response against the skin pathogen. Both the oral and topical administration of the UCO-SCM3 strain was capable of reducing the replication of C. acnes in skin lesions and beneficially modulating the inflammatory response. Of note, orally administered W. viridescens UCO-SMC3 induced more remarkable changes in the immune response to C. acnes than the topical treatment. However, the topical administration of W. viridescens UCO-SMC3 was more efficient than the oral treatment to reduce pathogen bacterial loads in the skin, and effects probably related to its ability to inhibit and antagonize the adhesion of C. acnes. Furthermore, a pilot study in acne volunteers demonstrated the capacity of a facial cream containing the UCO-SMC3 strain to reduce acne lesions. The results presented here encourage further mechanistic and clinical investigations to characterize W. viridescens UCO-SMC3 as a probiotic for acne vulgaris treatment.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 684 ◽  
Author(s):  
Christian Gorzelanny ◽  
Christian Mess ◽  
Stefan W. Schneider ◽  
Volker Huck ◽  
Johanna M. Brandner

Although, drugs are required in the various skin compartments such as viable epidermis, dermis, or hair follicles, to efficiently treat skin diseases, drug delivery into and across the skin is still challenging. An improved understanding of skin barrier physiology is mandatory to optimize drug penetration and permeation. The various barriers of the skin have to be known in detail, which means methods are needed to measure their functionality and outside-in or inside-out passage of molecules through the various barriers. In this review, we summarize our current knowledge about mechanical barriers, i.e., stratum corneum and tight junctions, in interfollicular epidermis, hair follicles and glands. Furthermore, we discuss the barrier properties of the basement membrane and dermal blood vessels. Barrier alterations found in skin of patients with atopic dermatitis are described. Finally, we critically compare the up-to-date applicability of several physical, biochemical and microscopic methods such as transepidermal water loss, impedance spectroscopy, Raman spectroscopy, immunohistochemical stainings, optical coherence microscopy and multiphoton microscopy to distinctly address the different barriers and to measure permeation through these barriers in vitro and in vivo.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 416 ◽  
Author(s):  
Schneider ◽  
Koziolek ◽  
Weitschies

More than 50 years ago, the first concepts for gastroretentive drug delivery systems were developed. Despite extensive research in this field, there is no single formulation concept for which reliable gastroretention has been demonstrated under different prandial conditions. Thus, gastroretention remains the holy grail of oral drug delivery. One of the major reasons for the various setbacks in this field is the lack of predictive in vitro and in vivo test methods used during preclinical development. In most cases, human gastrointestinal physiology is not properly considered, which leads to the application of inappropriate in vitro and animal models. Moreover, conditions in the stomach are often not fully understood. Important aspects such as the kinetics of fluid volumes, gastric pH or mechanical stresses have to be considered in a realistic manner, otherwise, the gastroretentive potential as well as drug release of novel formulations cannot be assessed correctly in preclinical studies. This review, therefore, highlights the most important aspects of human gastrointestinal physiology and discusses their potential implications for the evaluation of gastroretentive drug delivery systems.


2010 ◽  
Vol 8 (1) ◽  
pp. 225-238 ◽  
Author(s):  
Hong Yuan ◽  
Lin-Juan Lu ◽  
Yong-Zhong Du ◽  
Fu-Qiang Hu

1992 ◽  
Vol 19 (1-3) ◽  
pp. 131-144 ◽  
Author(s):  
Waleed S.W. Shalaby ◽  
William E. Blevins ◽  
Kinam Park

Author(s):  
Jayadeep R. Yadav ◽  
Swati C. Jagdale ◽  
Anuruddha R. Chabukswar

Background and Objective: Fluconazole (FLZ) is a novel triazole antifungistatic drug; topical administration of FLZ resulted in systemic absorption and skin inflammation, and thereby failed to achieve mycological eradication, resulting in low patient compliance and undermining therapy effectiveness. The aim of this study was to use the emulsion solvent evaporation technique to create FLZ-loaded nanosponges (NSs) using ethylcellulose (EC) and polyvinyl alcohol (PVA) as a stabiliser. Materials and Method: By varying the drug concentration (FLZ), EC, and PVA, four formulations were developed, each of which was then optimized through particle characterization (polydispersity index (PDI), scanning electron microscopy (SEM), zeta potential (ZP), drug entrapment, and loading efficiency). Results: SEM (Scanning Electron Microscope) analysis showed that the particle sizes of FLZ inclusion complexes ranged from 150 2 to 250 5 nm. The ZP was strong enough to produce stable formulations. FLZ was released from the nano sponges in a regulated manner for 24 hours in both in vitro and in vivo experiments. FTIR and DSC were used to validate the association of the FLZ with the nanosponges. The crystalline nature of FLZ was modified to an amorphous state due to the complexation with the nanosponges, according to an XRPD analysis. The FLZ nanosponges were found to be stable in a stability analysis. Conclusion: Therefore, ethyl cellulose-based nanosponges provide a novel method for controlling the release of FLZ for antifungal effects.


Nutrients ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 573 ◽  
Author(s):  
Hye Yang ◽  
Hyunkyoung Lee ◽  
Jong-Hyun Kim ◽  
Il-Hwa Hong ◽  
Du Hwang ◽  
...  

Rumex japonicus Houtt. (RJ) is traditionally used in folk medicines to treat patients suffering from skin disease in Korea and other parts of East Asia. However, the beneficial effect of RJ extract on atopic dermatitis (AD) has not been thoroughly examined. Therefore, this study aimed to investigate the anti-inflammatory effects of RJ on AD in vitro and in vivo. Treatment with RJ inhibited the phosphorylation of mitogen-activated protein kinase (MAPK) as well as the activation of nuclear factor-kappa B (NF-κB) in tumor necrosis factor-α (TNF-α) stimulated in HaCaT cells. The five-week-old Balb/c mice were used as an AD-like mouse model by treating them with 1-chloro-2, 4-dinitrobenzene (DNCB). Topical administration of RJ to DNCB-treated mice significantly reduced clinical dermatitis severity, epidermal thickness, and decreased mast cell and eosinophil infiltration into skin and ear tissue. These results suggest that RJ inhibits the development of AD-like skin lesions by regulating the skin inflammation responses in HaCaT cells and Balb/c mice. Thus, RJ may be a potential therapeutic agent for AD.


2017 ◽  
Vol 14 (3) ◽  
pp. 757-769 ◽  
Author(s):  
Mohammed S. Alqahtani ◽  
M. Saiful Islam ◽  
Satheesh Podaralla ◽  
Radhey S. Kaushik ◽  
Joshua Reineke ◽  
...  

Pharmaceutics ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 46
Author(s):  
Khaled M. Hosny ◽  
Khalid S. Al Nahyah ◽  
Nabil A. Alhakamy

Acne vulgaris is a common skin disease that affects everybody at least once in their lives. The treatment is challenging because the stratum corneum contains rigid corneocytes surrounded by intercellular lamellae that are difficult to bypass. In the present study, we intended to formulate an effective nanoemulsion that could deliver isotretinoin (ITT) with enhanced solubility, permeability, and bioavailability across the skin. ITT can have a serious hepatotoxic effect if given too frequently or erratically. Therefore, to overcome the aforesaid limitation, quercetin (QRS), a hepatoprotective agent, was incorporated into the formulation. Initially, the ITT solubility was determined in various surfactants and cosurfactants to select the essential ingredients to be used in the formulation and to optimize a nanoemulsion that could enhance the solubility and permeability of ITT and its antimicrobial activity against Staphyloccocus aureus, which is the main microorganism responsible for acne vulgaris. The mixture design was applied to study the interactions and optimize the independent variables that could match the prerequisites of selected dependent responses. A formulation containing 0.25 g of rosehip oil, 0.45 g of surfactant (Lauroglycol-90), and 0.3 g of cosurfactant (propylene glycol) was chosen as an optimized desirable formulation. The optimized batch was loaded with QRS and evaluated for in vitro and ex vivo permeation. The in vivo hepatotoxicity was assessed through topical administration. Permeability studies confirmed the enhanced permeation percentage of ITT (52.11 ± 2.85%) and QRS (25.44 ± 3.18%) of the optimized formulation, with an enhanced steady-state flux (Jss). The in vivo studies conducted on experimental animals demonstrated superior hepatoprotective activity of the prepared optimized formulation compared with other formulations of drugs and commercially marketed products. We anticipate that this optimized ITT formulation, followed up with good clinical evaluations, can be a breakthrough in the safe treatment of acne vulgaris.


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