Development of Microemulsion Dermal Products Based on Avocado Oil for Topical Administration

Background: 18β- glycyrrhetinic acid (Gly) is the major bioactive component of licorice roots and rhizomes of the Glycyrrhiza glabra species. It shows many activities such as antiviral, anti-inflammatory, antioxidant, antimicrobial, and antifungal, however, its use in the health field is very limited due to the low water solubility. Methods: This paper deals with the development of a new technological approach for Gly dissolution rate enhancement. It consists of Gly intercalation (guest) in the interlamellar spaces between the inorganic spaces (host) of the anionic clays “hydrotalcites” (HTlc) to obtain hybrids MgAl-HTlc-Gly and ZnAl-HTlc-Gly. Gly can find applications in both systemic and local therapies, thus advantages of the use of the hybrids in these two fields were investigated. Results: Gly dissolution rate from hybrids in the intestinal environment, site in which it is preferentially absorbed, resulted enhanced (ZnAl-HTlc-Gly > MgAl-HTlc-Gly) compared to the crystalline form, thereby, making them suitable for oral administration as dry powder in hard capsules. : For a local therapy, bioadhesive, vaginal emulgels loaded with the hybrids were developed. These showed suitable mucoadhesive property to the vaginal mucosa, necessary to prolong the residence time in the application site. The emulgel containing ZnAl-HTlc-Gly showed a faster and higher release profile than that containing MgAl- HTlc-Gly. Conclusions: The obtained results suggest that Gly intercalation into HTlc, especially in ZnAl-HTlc, allows to enhance Gly dissolution when the hybrids are formulated both as oral or topical products.

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Gel-based Microemulsion Design and Evaluation for Topical Application of Rivastigmine

Current Pharmaceutical Biotechnology ◽

10.2174/1389201020666191113144636 ◽

2020 ◽

Vol 21 (4) ◽

pp. 298-304

Author(s):

Chih-Wen Fang ◽

Ling-Chun Tsai ◽

Yaw-Syan Fu ◽

Ting-Yu Cheng ◽

Pao-Chu Wu

Keyword(s):

Topical Application ◽

Skin Irritation ◽

Topical Administration ◽

Lag Time ◽

Enhancement Effect ◽

Microemulsion Formulation ◽

Rat Skin ◽

Glycol Monobutyl Ether ◽

Loading Amount ◽

Hydrophilic Gel

Objective: The aim of the present study was to design nanocarriers for the topical application of rivastigmine. Methods: The effect of cosurfactants, hydrophilic gel and loading amount on the permeability of rivastigmine through rat skin was evaluated. Skin irritation tests and stability tests were performed to evaluate the utility of tested formulations. Results: The results showed that the microemulsion formation and characteristics of drug-loaded formulations were related to many parameters of the components. When using microemulsion systems as a vehicle, the permeation rate remarkably increased about 13.2~24.3-fold and the lag time was significantly shortened from 24 h to 4.7 h. Formulations containing a cosurfactant of Diethylene Glycol Monobutyl Ether (DEGBE) showed higher enhancement effect, while increasing the loading dose from 0.5% to 5% further increased the flux about 2.1-fold and shortened the lag time. Conclusion: The drug-loaded experimental formulation did not cause skin irritation and had good stability at 20ºC and 40ºC storage for at least 3 months. The result showed that gel-based microemulsion formulation could be a promising approach for topical administration.

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Improving Topical Skin Delivery of Monocrotaline Via Liposome Gel-based Nanosystems

Current Drug Delivery ◽

10.2174/1567201816666191029125300 ◽

2019 ◽

Vol 16 (10) ◽

pp. 940-950 ◽

Cited By ~ 1

Author(s):

Jiandong Yu ◽

Zhi Chen ◽

Yan-zhi Yin ◽

Chaoyuan Tang ◽

Enying Hu ◽

...

Keyword(s):

Gradient Method ◽

Encapsulation Efficiency ◽

Ph Value ◽

Topical Administration ◽

Ph Gradient ◽

Stability Factor ◽

Buffer Solution ◽

Skin Delivery ◽

Skin Retention

Background: In this study, a liposomal gel based on a pH-gradient method was used to increase the skin-layer retention of monocrotaline (MCT) for topical administration. Methods: Using the Box-Behnken design, different formulations were designed to form liposome suspensions with optimal encapsulation efficiency (EE%) and stability factor (KE). In order to keep MCT in liposomes and accumulate in skin slowly and selectively, MCT liposome suspensions were engineered into gels. Results: A pH-gradient method was used to prepare liposome suspensions. The optimal formulation of liposome suspensions (encapsulation efficiency: 83.10 ± 0.21%) was as follows: MCT 12 mg, soybean phosphatidyl choline (sbPC) 200 mg, cholesterol (CH) 41 mg, vitamin E (VE) 5 mg, and citric acid buffer solution (CBS) 4.0 10 mL (pH 7.0). The final formulation of liposomal gels consisted of 32 mL liposome suspensions, 4.76 mL deionized water, 0.40 g Carbopol-940, 1.6 g glycerol, 0.04 g methylparaben, and a suitable amount of triethanolamine for pH value adjustment. The results of in vitro drug release showed that MCT in liposomal gels could be released in 12 h constantly in physiological saline as a Ritger-Peppas model. Compared with plain MCT in gel form, liposomal MCT in gel had higher skin retention in vitro. Conclusion: In this study, liposomal gels were formed for greater skin retention of MCT. It is potentially beneficial for reducing toxicities of MCT by topical administration with liposomal gel.

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Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies

Pharmaceutics ◽

10.3390/pharmaceutics13040533 ◽

2021 ◽

Vol 13 (4) ◽

pp. 533

Author(s):

Eloy Pena-Rodríguez ◽

Maria Lajarin-Reinares ◽

Aida Mata-Ventosa ◽

Sandra Pérez-Torras ◽

Francisco Fernández-Campos

Keyword(s):

In Vitro Release ◽

Human Keratinocytes ◽

Topical Administration ◽

In Vitro Cytotoxicity ◽

Hair Follicles ◽

Vertical Diffusion ◽

Biodistribution Studies ◽

Follicular Targeting ◽

Depot Effect

Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated.

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Anti‐inflammatory effect of amygdalin analogs following topical administration on the TPA‐induced irritant contact dermatitis model in mice

Experimental Dermatology ◽

10.1111/exd.14284 ◽

2021 ◽

Author(s):

Monica Porras ◽

Lluis A. Gomez ◽

Juan J. Perez

Keyword(s):

Contact Dermatitis ◽

Topical Administration ◽

Irritant Contact Dermatitis ◽

Anti Inflammatory ◽

Inflammatory Effect

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Comprehensive Review of Knee Osteoarthritis Pharmacological Treatment and the Latest Professional Societies’ Guidelines

Pharmaceuticals ◽

10.3390/ph14030205 ◽

2021 ◽

Vol 14 (3) ◽

pp. 205

Author(s):

Dragan Primorac ◽

Vilim Molnar ◽

Vid Matišić ◽

Damir Hudetz ◽

Željko Jeleč ◽

...

Keyword(s):

Knee Osteoarthritis ◽

Platelet Rich Plasma ◽

Symptom Relief ◽

Topical Administration ◽

Symptomatic Therapy ◽

Therapy Options ◽

Professional Societies ◽

Inflammatory Drugs ◽

The Right

Osteoarthritis is the most common musculoskeletal progressive disease, with the knee as the most commonly affected joint in the human body. While several new medications are still under research, many symptomatic therapy options, such as analgesics (opioid and non-opioid), nonsteroid anti-inflammatory drugs, symptomatic slow-acting drugs in osteoarthritis, and preparations for topical administration, are being used, with a diverse clinical response and inconsistent conclusions across various professional societies guidelines. The concept of pharmacogenomic-guided therapy, which lies on principles of the right medication for the right patient in the right dose at the right time, can significantly increase the patient’s response to symptom relief therapy in knee osteoarthritis. Corticosteroid intra-articular injections and hyaluronic acid injections provoke numerous discussions and disagreements among different guidelines, even though they are currently used in daily clinical practice. Biological options, such as platelet-rich plasma and mesenchymal stem cell injections, have shown good results in the treatment of osteoarthritis symptoms, greatly increasing the patient’s quality of life, especially when combined with other therapeutic options. Non-inclusion of the latter therapies in the guidelines, and their inconsistent stance on numerous therapy options, requires larger and well-designed studies to examine the true effects of these therapies and update the existing guidelines.

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