scholarly journals Topical Administration of Cannabidiol: Influence of Vehicle-Related Aspects on Skin Permeation Process

2020 ◽  
Vol 13 (11) ◽  
pp. 337
Author(s):  
Antonella Casiraghi ◽  
Umberto M. Musazzi ◽  
Giorgio Centin ◽  
Silvia Franzè ◽  
Paola Minghetti
Keyword(s):  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
Skin Permeation ◽  
Topical Administration ◽  
Optimal Choice ◽  
Literature Evidence ◽  
Hildebrand Solubility Parameter ◽  
Hydrophilic Gel ◽  
Franz Diffusion Cells

Cannabidiol (CBD) is a non-psychoactive cannabinoid isolated from Cannabis sativa which, given its claimed beneficial properties and therapeutic potential, has lately aroused considerable attention from the scientific community. Starting from the little literature evidence, the main purpose of this study was to investigate the topical administration of CBD, with particular focus on the influence of vehicle-related aspects on the skin permeation process. This could provide useful information for the design of suitable drug delivery systems which could be used in developing topical medicines and cosmetics. In vitro human skin permeation studies were conducted using modified Franz diffusion cells to compare the performance of four solutions and two semisolid formulations. The Hildebrand solubility parameter was used to better understand the thermodynamic aspects implied in the partitioning process of the cannabinoid compound into the skin. It was interestingly found that a hydrophilic gel, mostly consisting of propylene glycol (79%, w/w), can be an optimal choice for the topical administration of CBD. Moreover, the feasibility of the preparation of CBD-loaded (trans)dermal patches, made with new printing technology, was also demonstrated.

scholarly journals Penetration of Chlorhexidine into Human Skin

2008 ◽  
Vol 52 (10) ◽  
pp. 3633-3636 ◽  
Author(s):  
T. J. Karpanen ◽  
T. Worthington ◽  
B. R. Conway ◽  
A. C. Hilton ◽  
T. S. J. Elliott ◽  
...  
Keyword(s):  
Human Skin ◽  
High Performance ◽  
Skin Permeation ◽  
Full Thickness ◽  
Alternative Strategies ◽  
Thickness Skin ◽  
Skin Antisepsis ◽  
Permeation Studies ◽  
Franz Diffusion Cells

ABSTRACT This study evaluated a model of skin permeation to determine the depth of delivery of chlorhexidine into full-thickness excised human skin following topical application of 2% (wt/vol) aqueous chlorhexidine digluconate. Skin permeation studies were performed on full-thickness human skin using Franz diffusion cells with exposure to chlorhexidine for 2 min, 30 min, and 24 h. The concentration of chlorhexidine extracted from skin sections was determined to a depth of 1,500 μm following serial sectioning of the skin using a microtome and analysis by high-performance liquid chromatography. Poor penetration of chlorhexidine into skin following 2-min and 30-min exposures to chlorhexidine was observed (0.157 ± 0.047 and 0.077 ± 0.015 μg/mg tissue within the top 100 μm), and levels of chlorhexidine were minimal at deeper skin depths (less than 0.002 μg/mg tissue below 300 μm). After 24 h of exposure, there was more chlorhexidine within the upper 100-μm sections (7.88 ± 1.37 μg/mg tissue); however, the levels remained low (less than 1 μg/mg tissue) at depths below 300 μm. There was no detectable penetration through the full-thickness skin. The model presented in this study can be used to assess the permeation of antiseptic agents through various layers of skin in vitro. Aqueous chlorhexidine demonstrated poor permeation into the deeper layers of the skin, which may restrict the efficacy of skin antisepsis with this agent. This study lays the foundation for further research in adopting alternative strategies for enhanced skin antisepsis in clinical practice.

scholarly journals Cannabinoids in cancer treatment: Therapeutic potential and legislation

2019 ◽  
Vol 19 (1) ◽  
pp. 14-23 ◽  
Author(s):  
Barbara Dariš ◽  
Mojca Tancer Verboten ◽  
Željko Knez ◽  
Polonca Ferk
Keyword(s):  
Cancer Treatment ◽  
Cancer Patients ◽  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
Herbal Remedy ◽  
Synthetic Cannabinoids ◽  
Cancer Type ◽  
Antitumor Effects ◽  
The Eu

The plant Cannabis sativa L. has been used as an herbal remedy for centuries and is the most important source of phytocannabinoids. The endocannabinoid system (ECS) consists of receptors, endogenous ligands (endocannabinoids) and metabolizing enzymes, and plays an important role in different physiological and pathological processes. Phytocannabinoids and synthetic cannabinoids can interact with the components of ECS or other cellular pathways and thus affect the development/progression of diseases, including cancer. In cancer patients, cannabinoids have primarily been used as a part of palliative care to alleviate pain, relieve nausea and stimulate appetite. In addition, numerous cell culture and animal studies showed antitumor effects of cannabinoids in various cancer types. Here we reviewed the literature on anticancer effects of plant-derived and synthetic cannabinoids, to better understand their mechanisms of action and role in cancer treatment. We also reviewed the current legislative updates on the use of cannabinoids for medical and therapeutic purposes, primarily in the EU countries. In vitro and in vivo cancer models show that cannabinoids can effectively modulate tumor growth, however, the antitumor effects appear to be largely dependent on cancer type and drug dose/concentration. Understanding how cannabinoids are able to regulate essential cellular processes involved in tumorigenesis, such as progression through the cell cycle, cell proliferation and cell death, as well as the interactions between cannabinoids and the immune system, are crucial for improving existing and developing new therapeutic approaches for cancer patients. The national legislation of the EU Member States defines the legal boundaries of permissible use of cannabinoids for medical and therapeutic purposes, however, these legislative guidelines may not be aligned with the current scientific knowledge.

scholarly journals Transdermal Nitroglycerin Delivery Using Acrylic Matrices: Design, Formulation, and In Vitro Characterization

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Houman Savoji ◽  
Amir Mehdizadeh ◽  
Ahmad Ramazani Saadat Abadi
Keyword(s):  
Skin Permeation ◽  
Peel Strength ◽  
Adhesion Properties ◽  
Pressure Sensitive Adhesives ◽  
In Vitro Characterization ◽  
Chemical Permeation Enhancers ◽  
Transdermal Drug Delivery Systems ◽  
Franz Diffusion Cells ◽  
Chemical Permeation

Nitroglycerin (TNG) transdermal drug delivery systems (TDDSs) with different acrylic pressure-sensitive adhesives (PSAs) and chemical permeation enhancers (CPEs) were prepared. The effects of PSAs and CPEs types and concentrations on skin permeation and in vitro drug release from devices were evaluated using the dissolution method as well as the modified-jacketed Franz diffusion cells fitted with excised rat abdominal skin. It was demonstrated that the permeation rate or steady state flux (Jss) of the drug through the excised rat skin was dependent on the viscosity and type of acrylic PSA as well as the type of CPE. Among different acrylic PSAs, Duro-Tak 2516 and Duro-Tak 2054 showed the highest and Duro-Tak 2051 showed the lowest Jss. Among the various CPEs, propylene glycol and cetyl alcohol showed the highest and the lowest enhancement of the skin permeation of TNG, respectively. The adhesion properties of devices such as 180° peel strength and probe tack values were obtained. It was shown that increasing the concentration of CPE led to reduction in the adhesion property of PSA. Moreover, after optimization of the formulation, it was found that the use of 10% PG as a CPE and 25% nitroglycerin loading in Duro-Tak 2054 is an effective monolithic DIAP for the development of a transdermal therapeutic system for nitroglycerin.

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 In vitro tissue culture and genetic analysis of two high-CBD medical cannabis (Cannabis sativa L.) breeding lines

Genetika ◽  
2020 ◽  
Vol 52 (3) ◽  
pp. 925-941 ◽  
Author(s):  
Spela Mestinsek-Mubi ◽  
Sinja Svetik ◽  
Marko Flajsman ◽  
Jana Murovec
Keyword(s):  
Tissue Culture ◽  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
Culture Media ◽  
Shoot Culture ◽  
Medical Cannabis ◽  
Breeding Lines ◽  
In Vitro Tissue Culture ◽  
Tissue Culture Media

The species Cannabis sativa L. has recently witnessed a resurgence of interest all over the world due to its multipurpose applications and the scientific confirmation of its pharmacological properties. Genotypes with high cannabinoid content are appreciated in the pharmaceutical and cosmetic industries due to their therapeutic potential. These genotypes, with predominantly high cannabidiol (CBD) content, are the subject of research and breeding in several programs, but to date, little data is published on the in vitro tissue culture of cannabis. Our study focused on the establishment of an efficient micropropagation method for two high-CBD breeding lines (MX-CBD-11 and MX-CBD-707) as the basis for advanced biotechnological breeding approaches. The results demonstrated that the in vitro culture of medical cannabis can be initiated on different culture media, that cultured plants can be successfully acclimatized, and that nodal position, and especially the genotype, have a significant influence on the success of shoot culture establishment. They showed that the published tissue culture media optimized for one high-THC strain of Mexican cannabis are not as efficient for other genotypes of (medical) cannabis. We complemented this research with a genetic study of 95 plants of the two breeding lines with 16 microsatellite (SSR) markers which clustered the plants based on breeding line. The results demonstrated that only 8 markers are needed for discrimination of all analyzed plants and their usefulness for clonal identification.

scholarly journals Cannabidiol Signaling in the Eye and Its Potential as an Ocular Therapeutic Agent

2021 ◽  
Vol 55 (S5) ◽  
pp. 1-14
Keyword(s):  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
In Vivo Studies ◽  
Future Directions ◽  
Clinical Drug Development ◽  
Therapeutic Uses ◽  
The 1960S ◽  
Clinical Drug

Cannabidiol (CBD), the major non-intoxicating constituent of Cannabis sativa, has gained recent attention due to its putative therapeutic uses for a wide variety of diseases. CBD was discovered in the 1940s and its structure fully characterized in the 1960s. However, for many years most research efforts related to cannabis derived chemicals have focused on D9-tetrahydrocannabinol (THC). In contrast to THC, the lack of intoxicating psychoactivity associated with CBD highlights the potential of this cannabinoid for clinical drug development. This review details in vitro and in vivo studies of CBD related to the eye, the therapeutic potential of cannabidiol for various ocular conditions, and molecular targets and mechanisms for CBD-induced ocular effects. In addition, challenges of CBD applications for clinical ocular therapeutics and future directions are discussed.

scholarly journals Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Saleh A. Al-Suwayeh ◽  
Ehab I. Taha ◽  
Fahad M. Al-Qahtani ◽  
Mahrous O. Ahmed ◽  
Mohamed M. Badran
Keyword(s):  
Analgesic Activity ◽  
Skin Permeation ◽  
Tween 80 ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Topical Gel ◽  
Carbopol Gel ◽  
Franz Diffusion Cells ◽  
Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

scholarly journals Cannabis sativa and Skin Health: Dissecting the Role of Phytocannabinoids

Planta Medica ◽  
2021 ◽  
Author(s):  
Giulia Martinelli ◽  
Andrea Magnavacca ◽  
Marco Fumagalli ◽  
Mario DellʼAgli ◽  
Stefano Piazza ◽  
...  
Keyword(s):  
Clinical Studies ◽  
Skin Diseases ◽  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
Current Evidence ◽  
Skin Disorders ◽  
Anti Inflammatory

AbstractThe use of Cannabis sativa is currently recognized to ease certain types of chronic pain, reduce chemotherapy-induced nausea, and improve anxiety. Nevertheless, few studies highlighted the therapeutic potential of C. sativa extracts and related phytocannabinoids for a variety of widespread skin disorders including acne, atopic dermatitis, psoriasis, pruritus, and pain. This review summarized the current evidence on the effects of phytocannabinoids at the cutaneous level through the collection of in vitro, in vivo, and clinical studies published on PubMed, Scopus, Embase, and Web of Science until October 2020. Phytocannabinoids have demonstrated potential anti-inflammatory, antioxidant, anti-aging, and anti-acne properties by various mechanisms involving either CB1/2-dependent and independent pathways. Not only classical immune cells, but also several skin-specific actors, such as keratinocytes, fibroblasts, melanocytes, and sebocytes, may represent a target for phytocannabinoids. Cannabidiol, the most investigated compound, revealed photoprotective, antioxidant, and anti-inflammatory mechanisms at the cutaneous level, while the possible impact on cell differentiation, especially in the case of psoriasis, would require further investigation. Animal models and pilot clinical studies supported the application of cannabidiol in inflammatory-based skin diseases. Also, one of the most promising applications of non-psychotropic phytocannabinoids is the treatment of seborrheic disorders, especially acne. In conclusion, the incomplete knowledge of the role of the endocannabinoid system in skin disorders emerged as an important limit for pharmacological investigations. Moreover, the limited studies conducted on C. sativa extracts suggested a higher potency than single phytocannabinoids, thus stimulating new research on phytocannabinoid interaction.

Formulation and Evaluation of DHA Oil based Nicotinamide Nanoemulsion Gel for Treating Atopic Dermatitis

2020 ◽  
Vol 10 (6) ◽  
pp. 892-901
Author(s):  
Gayathri P. Pradeep ◽  
Vidya Viswanad
Keyword(s):  
Drug Release ◽  
Cell Line ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Nanoemulsion Gel ◽  
Permeation Studies ◽  
Franz Diffusion Cells

Background: Atopic dermatitis (or eczema) can be defined as a chronic inflammatory condition accompanied by severe pruritus. Objective: The prepared gel was evaluated for in vitro drug release, in vitro occlusion studies, transepidermal water loss studies, skin permeation studies, in vitro skin irritation studies and antiinflammatory cell line studies. Methods: In vitro drug release studies were performed using Franz diffusion cells. The in vitro occlusion studies were carried out by the procedure reported by Wissing et al. TEWL determination was done by the method proposed by Reiger. The skin permeation studies were carried out using porcine skin using Franz diffusion cells. In vitro skin irritation study was carried out using HETCAM (Hen’s Egg Test on the Chorioallantoic Membrane) method. Anti-inflammatory cell line studies were carried out using RAW 264.7 cell lines. Results: In vitro drug release studies,drug release of nicotinamide from nanoemulsion gel was found to be more than marketed gel. Kinetic modelling showed a higuchi model with non-fickian diffusion. In vitro occlusion study showed the percentage of evaporated water from prepared nanoemulsion formulation after 72 h is very less compared with the other formulations. The TEWL measurement shows the reduction in TEWL has more in prepared nanoemulsion gel than other formulations. Anti-inflammatory cell line studies proved that the nanoemulsion gel has inhibition capacity on COX activity, LOX activity, Inducibe nitric oxide synthase and cellular nitrate levels. Conclusion: DHA oil based nicotinamidenanoemulsion gel were prepared successfully and the evaluation of prepared gel showed better drug release and skin permeation with better antiinflammatory activity.

scholarly journals Increased Therapeutic Efficacy of SLN Containing Etofenamate and Ibuprofen in Topical Treatment of Inflammation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 328
Author(s):  
Giuliana Mancini ◽  
Lídia M. D. Gonçalves ◽  
Joana Marto ◽  
Filomena A. Carvalho ◽  
Sandra Simões ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Hydroxypropyl Methylcellulose ◽  
Liquid Molecule ◽  
Solid Lipid ◽  
Rat Paw Edema ◽  
In Vitro Permeation ◽  
Rat Paw ◽  
Franz Diffusion Cells

Innovative formulations, including solid lipid nanoparticles (SLNs), have been sought to improve skin permeation of non-steroidal anti-inflammatory drugs (NSAIDs). The present study explores the use of SLNs, prepared using a fusion-emulsification method, to increase skin permeation and in vivo activity of two relevant NSAIDs: A liquid molecule (etofenamate) and a solid one (ibuprofen), formulated in a 2% hydroxypropyl methylcellulose gel through the gelation of SLN suspensions. Compritol® 888 ATO and Tween® 80 were used as a solid lipid and a surfactant, respectively. All production steps were up scalable, resulting in SLNs with high encapsulation efficiency (>90%), a mean particle size of <250 nm, a polydispersity index <0.2, and that were stable for 12 months. In vitro permeation, using human skin in Franz diffusion cells, showed increased permeation and similar cell viability in Df and HaCaT cell lines for SLN formulations when compared to commercial formulations of etofenamate (Reumon® Gel 5%) and ibuprofen (Ozonol® 5%). In vivo activity in the rat paw edema inflammation model showed that SLN hydrogels containing lower doses of etofenamate (8.3 times lower) and ibuprofen (16.6 times lower) produced similar effects compared to the commercial formulations, while decreasing edema and inflammatory cell infiltration, and causing no histological changes in the epidermis. These studies demonstrate that encapsulation in SLNs associated to a suitable hydrogel is a promising technological approach to NSAIDs dermal application.

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