scholarly journals A Comprehensive Review on Natural Products as Chemical Penetration Enhancer

2021 ◽  
Vol 11 (5-S) ◽  
pp. 176-187
Author(s):  
Sudip Das ◽  
Koushik Sen Gupta
Keyword(s):  
Drug Delivery ◽  
Natural Products ◽  
Transdermal Drug Delivery ◽  
Skin Irritation ◽  
Penetration Enhancer ◽  
Penetration Enhancers ◽  
Topical Drug Delivery ◽  
Permeation Enhancers ◽  
In Vivo Models

The drug delivery within the stratum corneum of the skin prevails a challenging area for the pharmaceutical field, especially to the formulation scientists. Several investigations revealed that the lipid domain, which is the integral component of the transport barrier, must be breached if it is to be delivered transdermally at an appropriate rate. In particular, transdermal drug delivery has intrigued researchers with multiple suggestions because multiple dosing or insufficient drug delivery or characteristics of various drugs often results in low therapeutic effects. The application of permeation or penetration enhancers may prolong the number of drugs that can be offered topically. The application of any natural permeation enhancer is innoxious over the artificial permeation enhancers. The natural permeation enhancers are investigated, so notably include essential oils, terpenes, terpenoids, fatty acid esters, etc., have a certain effect in the transdermal drug delivery system. Despite decades of investigation on the natural chemical penetration enhancer, the researchers could not establish the effectiveness of natural penetration enhancers clinically due to the lack of in vivo models. Several factors, like solubility, solvent selection, experimental models, etc., has restricted the application and development of natural penetration enhancers in topical drug delivery systems, especially in the patches. Therefore, further investigation needs to do on skin irritation to decide natural penetration enhancers controlling optimum enhancement effects with minimal skin irritation. This review gives a comprehensive literature survey on naturally obtained chemical penetration enhancers and their future possibilities. Keywords: Topical Drug delivery system, Natural products, Penetration enhancer, Stratum corneum, In vivo models.

scholarly journals Improved Biosafety and Transdermal Delivery of Aconitine via Diethylene Glycol Monoethyl Ether-Mediated Microemulsion Assisted with Microneedles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 163 ◽  
Author(s):  
Yongtai Zhang ◽  
Hongmei Hu ◽  
Qian Jing ◽  
Zhi Wang ◽  
Zehui He ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Diethylene Glycol ◽  
Transdermal Drug Delivery ◽  
Skin Irritation ◽  
In Vivo Microdialysis ◽  
Monoethyl Ether ◽  
Glycol Monoethyl Ether ◽  
Diethylene Glycol Monoethyl Ether

In the current study, diethylene glycol monoethyl ether-mediated microemulsions were combined with microneedles for enhanced transdermal aconitine delivery. The oil-in-water microemulsion increasedaconitine solubility and enhanced transdermal drug delivery and assistance with metal microneedles enhanced permeation of the aconitine-loaded microemulsion. Carried by the microemulsion, the in vitro permeability of aconitine was significantly enhanced, and further improved using microneedles. In vivo microdialysis revealed that the subcutaneous local drug concentration reached a high level within 30 min and remained relatively consistent to the end of the experimental period. AUC0-t of the microemulsion group was significantly higher than that of the aqueous solution group, and the microemulsion combined with microneedles group achieved the highest AUC0-t among the tested groups. The microemulsion and microdialysis probe also showed good biocompatibility with skin tissue. The microemulsion could be internalized by HaCaT and CCC-ESF-1 cells via lysosomes. The in vitro cytotoxicity of aconitine toward skin cells was reduced via encapsulation by microemulsion, and the prepared microemulsion developed no skin irritation. Hence, transdermal aconitine delivery and drug biosafety were effectively improved by loading into the microemulsion and assisting with microneedles, and in vivo microdialysis technique is suitable for realtime monitoring of transdermal drug delivery with microemulsion-based drug vehicles.

scholarly journals Elastic and Ultradeformable Liposomes for Transdermal Delivery of Active Pharmaceutical Ingredients (APIs)

2021 ◽  
Vol 22 (18) ◽  
pp. 9743
Author(s):  
Eliana B. Souto ◽  
Ana S. Macedo ◽  
João Dias-Ferreira ◽  
Amanda Cano ◽  
Aleksandra Zielińska ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Transdermal Delivery ◽  
Transdermal Drug Delivery ◽  
Drug Delivery Systems ◽  
First Generation ◽  
Delivery Systems ◽  
Topical Drug Delivery ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients

Administration of active pharmaceutical ingredients (APIs) through the skin, by means of topical drug delivery systems, is an advanced therapeutic approach. As the skin is the largest organ of the human body, primarily acting as a natural protective barrier against permeation of xenobiotics, specific strategies to overcome this barrier are needed. Liposomes are nanometric-sized delivery systems composed of phospholipids, which are key components of cell membranes, making liposomes well tolerated and devoid of toxicity. As their lipid compositions are similar to those of the skin, liposomes are used as topical, dermal, and transdermal delivery systems. However, permeation of the first generation of liposomes through the skin posed some limitations; thus, a second generation of liposomes has emerged, overcoming permeability problems. Various mechanisms of permeation/penetration of elastic/ultra-deformable liposomes into the skin have been proposed; however, debate continues on their extent/mechanisms of permeation/penetration. In vivo bioavailability of an API administered in the form of ultra-deformable liposomes is similar to the bioavailability achieved when the same API is administered in the form of a solution by subcutaneous or epi-cutaneous injection, which demonstrates their applicability in transdermal drug delivery.

scholarly journals Effects of Sting Plant Extracts as Penetration Enhancers on Transdermal Delivery of Hypoglycemic Compounds

Medicina ◽  
2019 ◽  
Vol 55 (5) ◽  
pp. 121
Author(s):  
Yuh-Ming Fuh ◽  
Dinh-Chuong Pham ◽  
Ching-Feng Weng
Keyword(s):  
Drug Delivery ◽  
Plant Extracts ◽  
Skin Permeation ◽  
Skin Irritation ◽  
Mouse Skin ◽  
Penetration Enhancers ◽  
Permeability Barrier ◽  
Trypan Blue Exclusion ◽  
Insulin Sensitizers

Background and objectives: The percutaneous route is an interesting and inventive investigation field of drug delivery. However, it is challenging for drug molecules to pass through the skins surface, which is a characterized by its permeability barrier. The purpose of this study is to look at the effect of some penetration enhancers on in vivo permeation of insulin and insulin sensitizers (curcumin and rutin) through diabetes-induced mouse skin. Materials and Methods: Sting crude extracts of Dendrocnide meyeniana, Urtica thunbergiana Sieb. and Zucc, and Alocasia odora (Lodd.) Spach were used as the penetration enhancers. Mouse skin irritation was tested by smearing the enhancers for the measurements at different time points and the cell viability of the HaCaT human skin keratinocytes, which was determined by Trypan blue exclusion and MTT assays to evaluate human biosafety for these extracts after the mouse skin permeation experiments. Results: All enhancers induced a slight erythema without edema on the mouse skin that completely recovered after 6 h from the enhancer smears as compared with normal mouse skin. Furthermore, no damaged cells were found in the HaCaT keratinocytes under sting crude extract treatments. The blood sugar level in the diabetic mice treated with the insulin or insulin sensitizers, decreased significantly (p < 0.05) in the presence of enhancers. The area under the curve (AUC) values of transdermal drug delivery (TDD) ranged from 42,000 ± 5000 mg/dL x min without enhancers, to 30,000 ± 2000 mg/dL x min in the presence of enhancers. Conclusions: This study exhibited that natural plant extracts could be preferred over the chemically synthesized molecules and are safe and potent penetration enhancers for stimulating the transdermal absorption of drugs.

scholarly journals A Review on Chemical Permeation Enhancers used in the Formulation of Transdermal Drug Delivery System

2021 ◽  
pp. 429-437
Author(s):  
. Shivani ◽  
Ritika Puri
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Free Water ◽  
Skin Barrier ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Permeation Enhancers ◽  
Transdermal Drug Delivery System ◽  
Chemical Permeation Enhancers ◽  
Chemical Permeation

Skin penetration enhancement technology is a rapidly evolving area that will greatly increase the quantity of transdermal drug delivery medications. Penetration enhancers are used to facilitate the movement of drugs through the skin barrier. Numerous methods exist for extending partition enhancement. The enhancers' contact with the polar head of the lipid groups is the potential means for increasing the penetration. Penetration enhancers improve the amount of free water molecules between the bilayer, leading to an improvement of the polar drug diffusion cross section. This article focuses on the different compounds assessed for improving penetration activity like sulphoxides, azones, pyrrolidones, alcohols and alkanols, glycols, surfactants and terpenes.

scholarly journals CHEMICAL PENETRATION ENHANCERS FOR TRANSDERMAL DRUG DELIVERY SYSTEM

2018 ◽  
Vol 8 (5-s) ◽  
pp. 62-66 ◽  
Author(s):  
Anupriya Kapoor ◽  
Shashi Kiran Mishra ◽  
Dharmesh Kumar Verma ◽  
Prashant Pandey
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Systemic Circulation ◽  
Oral Route ◽  
Penetration Enhancer ◽  
Penetration Enhancers ◽  
Transdermal Drug Delivery System ◽  
Transdermal Patches

In present scenario more than 70% of the drugs that are taken by oral route are found to be less effective as desired, to overcome this constraint Transdermal drug delivery system has emerged as an innovative area of research, this system helps in delivering the drugs and macromolecules through skin into systemic circulation. At present, the worldwide market of Transdermal patch has reached 2 billion pounds. Many drugs like Estrogen, Progestrone, Nitroglycerine, Clonodine etc. are fabricated in form of Transdermal patches due to its ability to deliver the drug in non-invasive manner and also to overcome the problems associated with oral route. Although the Transdermal patches deliver the drug at predetermined rate1, the partitioning of drug from the system to the skin and then penetration through different layers of skin can be altered by adding penetration enhancers that can be physical or chemical in nature. This article deals with the role of different chemicals that can be used as penetration enhancer. Keywords: Penetration enhancer, Layer of skin, Fatty alcohol and glycol

Potential for Treatment of Neurodegenerative Diseases with Natural Products or Synthetic Compounds that Stabilize Microtubules

2020 ◽  
Vol 26 (35) ◽  
pp. 4362-4372
Author(s):  
John H. Miller ◽  
Viswanath Das
Keyword(s):  
Natural Products ◽  
Neurodegenerative Diseases ◽  
In Vivo Models ◽  
Synthetic Compounds ◽  
Stabilizing Agents ◽  
Animal Models Of Disease ◽  
Model Studies ◽  
Models Of Disease

No effective therapeutics to treat neurodegenerative diseases exist, despite significant attempts to find drugs that can reduce or rescue the debilitating symptoms of tauopathies such as Alzheimer’s disease, Parkinson’s disease, frontotemporal dementia, amyotrophic lateral sclerosis, or Pick’s disease. A number of in vitro and in vivo models exist for studying neurodegenerative diseases, including cell models employing induced-pluripotent stem cells, cerebral organoids, and animal models of disease. Recent research has focused on microtubulestabilizing agents, either natural products or synthetic compounds that can prevent the axonal destruction caused by tau protein pathologies. Although promising results have come from animal model studies using brainpenetrant natural product microtubule-stabilizing agents, such as paclitaxel analogs that can access the brain, epothilones B and D, and other synthetic compounds such as davunetide or the triazolopyrimidines, early clinical trials in humans have been disappointing. This review aims to summarize the research that has been carried out in this area and discuss the potential for the future development of an effective microtubule stabilizing drug to treat neurodegenerative disease.

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