scholarly journals IONTOPHORESIS: A FUNCTIONAL APPROACH FOR ENHANCEMENT OF TRANSDERMAL DRUG DELIVERY

Author(s):  
Sanjoy De ◽  
Souvik Mallik ◽  
Sabuj Kumar Bhattacharya ◽  
Shibam Acharya ◽  
Partha Sarathi Mondal ◽  
...  

Iontophoresis is one of the most widely studied active techniques for enhancing transdermal delivery of drugs. However, its ability to enhance the delivery of highly lipophilic compounds is poor due to lack of any charge and poor water solubility of molecules. The skin has been used as a port for systemic delivery of therapeutic agents since several decades. The composition of stratum corneum renders it a daunting barrier to the topical and transdermal administration of therapeutic agents. The number of drug molecules for transdermal delivery is limited owing to the physicochemical restrictions. The delivery of drugs into systemic circulation via skin has generated much attention during the last decade. Transdermal therapeutic systems propound controlled release of active ingredients through the skin and into the systemic circulation in a predictive manner. Drugs administered through these systems escape first-pass metabolism and maintain a steady state scenario similar to a continuous intravenous infusion for up to several days. Keywords: Iontophoresis, non-invasive, stratum corneum, acid-alkaline reaction, chemical permeation enhancer, reverse iontophoresis.

1997 ◽  
Vol 2 (2) ◽  
pp. 108-119 ◽  
Author(s):  
Virginia Merino ◽  
Ingo Alberti ◽  
Yogeshvar N. Kalia ◽  
Richard H. Guy

Background: The application of therapeutic agents to the skin addresses three general objectives: (a) the treatment of a variety of dermatologic diseases; (b) the “targeted” delivery of drugs to deeper subcutaneous tissues, with a concomitant reduction in systemic exposure; and (c) socalled transdermal administration to elicit a systemic pharmacologic effect. Objective: Recently, significant progress towards all three goals has been recorded and the level of research and development activity remains high. We aim to discuss these advances from mechanistic and clinical standpoints. Results: For the topical treatment of skin disease, novel vehicles (e.g., stabilized, supersaturated systems and liposomal formulations) have led to dramatic improvements in local drug bioavailability. Transdermal delivery of drugs for systemic effect, though limited in terms of the number of compounds, is perhaps the most commercially successful (in terms of the number of products) of the controlled release technologies. Considerable activity continues to enhance drug delivery (and hence to extend the range of drugs for which transdermal delivery can be used). Existing patches use formulations that contain solvents and adjuvants capable of reducing the barrier function of the skin. Much effort is directed at iontophoresis (electrically enhanced transport), particularly for small peptides that are difficult to administer by other routes. “Reverse iontophoresis” may allow the extraction of glucose (without skin puncture) so that continuous, noninvasive monitoring of blood sugar in diabetics approaches realization. Conclusion: In the not too distant future, the skin may also play a role not only in drug delivery, but also with respect to measurements in clinical chemistry.


Author(s):  
Ms Chetna

The Skin is one of the most extensive organs of the human body. This multilayered organ receives approximately one-third of all blood circulating through body. With a thickness of about a millimeter, the skin separates the underlying blood circulation network from the outside environment1. Transdermal delivery of drugs through the skin to the systemic circulation provides a convenient route of administration for a variety of clinical indications. Transdermal delivery systems are currently available containing scopolamine (hyoscine) for motion sickness, clonidine and nitroglycerin for cardiovascular disease, fentanyl for chronic pain, nicotine to aid smoking cessation2. Drug molecules in contact with the skin surface can penetrate by three potential pathways: through the sweat ducts, via the hair follicles and sebaceous glands (collectively called the shunt or appendageal route), or directly across the stratum corneum3.   All transdermal drug delivery systems consist mainly of: Polymer matrix Drug Enhancers and other excipients Other excipient


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Tadashi Hattori ◽  
Hiroki Tagawa ◽  
Makoto Inai ◽  
Toshiyuki Kan ◽  
Shin-ichiro Kimura ◽  
...  

AbstractNobiletin (NOB), a flavonoid, has extremely low water solubility and low oral bioavailability; however, despite these problems, various physiological effects have been investigated in vitro. In the present study, we investigated the transdermal delivery of NOB using choline and geranic acid (CAGE), which is a biocompatible material that has been reported to be a promising transdermal delivery approach. The feasibility was evaluated by a set of in vitro and in vivo tests. A solubility evaluation demonstrated that CAGE induced excellent solubility of NOB induced by multipoint hydrogen bonding between NOB and CAGE. In vitro transdermal tests using a Franz diffusion cell showed that CAGE was effective in enhancing transdermal absorption of NOB, compared to other penetration enhancers. Subsequent in vivo tests demonstrated that CAGE significantly improved area under the concentration-time curve of NOB in vivo and NOB/CAGE sample showed 20-times higher bioavailability than oral administration of NOB crystal. Furthermore, NOB/CAGE sample also showed significant drops of the blood glucose level in rats derived from hypoglycemic activity of NOB. Thus, transdermal administration of NOB using CAGE was shown to be feasible, which indicates that the use of CAGE may be adapted for other flavonoids that also show both low water solubility and low permeability.


Author(s):  
Yi-Qun Yu ◽  
Xue Yang ◽  
Xiao-Fang Wu ◽  
Yi-Bin Fan

The transdermal route of administration provides numerous advantages over conventional routes i.e., oral or injectable for the treatment of different diseases and cosmetics applications. The skin also works as a reservoir, thus deliver the penetrated drug for more extended periods in a sustained manner. It reduces toxicity and local irritation due to multiple sites for absorption and owes the option of avoiding systemic side effects. However, the transdermal route of delivery for many drugs is limited since very few drugs can be delivered at a viable rate using this route. The stratum corneum of skin works as an effective barrier, limiting most drugs’ penetration posing difficulty to cross through the skin. Fortunately, some non-invasive methods can significantly enhance the penetration of drugs through this barrier. The use of nanocarriers for increasing the range of available drugs for the transdermal delivery has emerged as a valuable and exciting alternative. Both the lipophilic and hydrophilic drugs can be delivered via a range of nanocarriers through the stratum corneum with the possibility of having local or systemic effects to treat various diseases. In this review, the skin structure and major obstacle for transdermal drug delivery, different nanocarriers used for transdermal delivery, i.e., nanoparticles, ethosomes, dendrimers, liposomes, etc., have been discussed. Some recent examples of the combination of nanocarrier and physical methods, including iontophoresis, ultrasound, laser, and microneedles, have also been discussed for improving the therapeutic efficacy of transdermal drugs. Limitations and future perspectives of nanocarriers for transdermal drug delivery have been summarized at the end of this manuscript.


Polymers ◽  
2021 ◽  
Vol 13 (16) ◽  
pp. 2623
Author(s):  
Shubham Sharma ◽  
P. Sudhakara ◽  
Jujhar Singh ◽  
R. A. Ilyas ◽  
M. R. M. Asyraf ◽  
...  

In the determination of the bioavailability of drugs administered orally, the drugs’ solubility and permeability play a crucial role. For absorption of drug molecules and production of a pharmacological response, solubility is an important parameter that defines the concentration of the drug in systemic circulation. It is a challenging task to improve the oral bioavailability of drugs that have poor water solubility. Most drug molecules are either poorly soluble or insoluble in aqueous environments. Polymer nanocomposites are combinations of two or more different materials that possess unique characteristics and are fused together with sufficient energy in such a manner that the resultant material will have the best properties of both materials. These polymeric materials (biodegradable and other naturally bioactive polymers) are comprised of nanosized particles in a composition of other materials. A systematic search was carried out on Web of Science and SCOPUS using different keywords, and 485 records were found. After the screening and eligibility process, 88 journal articles were found to be eligible, and hence selected to be reviewed and analyzed. Biocompatible and biodegradable materials have emerged in the manufacture of therapeutic and pharmacologic devices, such as impermanent implantation and 3D scaffolds for tissue regeneration and biomedical applications. Substantial effort has been made in the usage of bio-based polymers for potential pharmacologic and biomedical purposes, including targeted deliveries and drug carriers for regulated drug release. These implementations necessitate unique physicochemical and pharmacokinetic, microbiological, metabolic, and degradation characteristics of the materials in order to provide prolific therapeutic treatments. As a result, a broadly diverse spectrum of natural or artificially synthesized polymers capable of enzymatic hydrolysis, hydrolyzing, or enzyme decomposition are being explored for biomedical purposes. This summary examines the contemporary status of biodegradable naturally and synthetically derived polymers for biomedical fields, such as tissue engineering, regenerative medicine, bioengineering, targeted drug discovery and delivery, implantation, and wound repair and healing. This review presents an insight into a number of the commonly used tissue engineering applications, including drug delivery carrier systems, demonstrated in the recent findings. Due to the inherent remarkable properties of biodegradable and bioactive polymers, such as their antimicrobial, antitumor, anti-inflammatory, and anticancer activities, certain materials have gained significant interest in recent years. These systems are also actively being researched to improve therapeutic activity and mitigate adverse consequences. In this article, we also present the main drug delivery systems reported in the literature and the main methods available to impregnate the polymeric scaffolds with drugs, their properties, and their respective benefits for tissue engineering.


2021 ◽  
Vol 11 (2) ◽  
pp. 113-120
Author(s):  
Neha Sharma ◽  
Tarun Kumar Sharma ◽  
Vinay Pandit ◽  
M. S Ashawat

Transdermal drug delivery system used to transport the drug across the skin deep into systemic circulation. The main advantages of Transdermal drug delivery system improved patient compliance, sustained release, avoidance of gastric irritation, as well as elimination of pre-systemic first-pass effect. But most of therapeutic agents is limited due to thickness of stratum corneum, which act as a barrier for the delivery of various drug molecules and only few molecules are able to reach the action site. Microneedles are the new form of delivery system, which are used to increase the delivery of drug through this route and overcoming the number of problems related to conventional drug delivery system the main aim of this review to focus on new innovation in transdermal drug delivery systems. In the microneedle drug delivery system, the skin is temporarily broken, that creating micron size pathways that deliver the sufficient amount of drug directly into the stratum corneum from which the drug can directly go into the systemic circulation. In this review, we describe different type of microneedles can be solid, coated, dissolving and biodegradable microneedles and their method of fabrication. Microneedles can be manufactured in different forms like hollow, solid, and dissolving. Also describe materials used for fabrication, fabrication techniques, methodology of drug delivery such as Poke and patch, Coat and poke, Poke and release, Poke and flow and evaluation parameters.


2020 ◽  
pp. 7-24
Author(s):  
Zhanna Kozlova ◽  
Ivan Krasnyuk ◽  
Yuliya Lebedeva ◽  
Ekaterina Odintsova

Oral mucosal drug delivery is an alternative method of systemic delivery with several advantages over both injectable and enteral methods. Drugs that are absorbed through the oral mucosa directly enter the systemic circulation, passing through the gastrointestinal tract and first-pass metabolism in the liver due to oral mucosa being highly vascularised. This results in rapid onset of action for some drugs because of a more comfortable and convenient way of delivery than the intravenous one. But not all drugs can be administered through the oral mucosa due to characteristics of the oral mucosa and physical and chemical properties of the drug.


2020 ◽  
Vol 20 (10) ◽  
pp. 1682-1695
Author(s):  
Foziyah Zakir ◽  
Kanchan Kohli ◽  
Farhan J. Ahmad ◽  
Zeenat Iqbal ◽  
Adil Ahmad

Osteoporosis is a progressive bone disease that remains unnoticed until a fracture occurs. It is more predominant in the older age population, particularly in females due to reduced estrogen levels and ultimately limited calcium absorption. The cost burden of treating osteoporotic fractures is too high, therefore, primary focus should be treatment at an early stage. Most of the marketed drugs are available as oral delivery dosage forms. The complications, as well as patient non-compliance, limit the use of oral therapy for prolonged drug delivery. Transdermal delivery systems seem to be a promising approach for the delivery of anti-osteoporotic active moieties. One of the confronting barriers is the passage of drugs through the SC layers followed by penetration to deeper dermal layers. The review focuses on how anti-osteoporotic drugs can be molded through different approaches so that they can be exploited for the skin to systemic delivery. Insights into the various challenges in transdermal delivery and how the novel delivery system can be used to overcome these have also been detailed.


2020 ◽  
Vol 15 (3) ◽  
pp. 1934578X1990068
Author(s):  
Noriyuki Uchida ◽  
Masayoshi Yanagi ◽  
Hiroki Hamada

Composite nanoparticles composed of an anionic phospholipid of 1,2-dipalmitoyl-sn-glycero-3-phosphorylglycerol (DPPG) and paclitaxel (PTX) were successfully prepared by mixing them in water followed by a subsequent heating/cooling process. The size of DPPG-PTX nanoparticle could be easily tuned by ultrasonic fragmentation. Upon addition of small-sized fluorescently labeled paclitaxel (FLPTX) nanoparticles with DPPG (DPPG-FLPTX) to rat skin tissue, part of the FLPTX molecules permeated to the stratum corneum.


2021 ◽  
Vol 10 (2) ◽  
pp. 181
Author(s):  
Vahid Alimardani ◽  
Samira Sadat Abolmaali ◽  
Gholamhossein Yousefi ◽  
Zahra Rahiminezhad ◽  
Mehdi Abedi ◽  
...  

Organic and inorganic nanoparticles (NPs) have shown promising outcomes in transdermal drug delivery. NPs can not only enhance the skin penetration of small/biomacromolecule therapeutic agents but can also impart control over drug release or target impaired tissue. Thanks to their unique optical, photothermal, and superparamagnetic features, NPs have been also utilized for the treatment of skin disorders, imaging, and biosensing applications. Despite the widespread transdermal applications of NPs, their delivery across the stratum corneum, which is the main skin barrier, has remained challenging. Microneedle array (MN) technology has recently revealed promising outcomes in the delivery of various formulations, especially NPs to deliver both hydrophilic and hydrophobic therapeutic agents. The present work reviews the advancements in the application of MNs and NPs for an effective transdermal delivery of a wide range of therapeutics in cancer chemotherapy and immunotherapy, photothermal and photodynamic therapy, peptide/protein vaccination, and the gene therapy of various diseases. In addition, this paper provides an overall insight on MNs’ challenges and summarizes the recent achievements in clinical trials with future outlooks on the transdermal delivery of a wide range of nanomedicines.


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