Fenugreek
Dilip Ghosh, Prasad Thakurdesai in Fenugreek, 2022
A transdermal patch is designed to release a controlled dose of a drug through the skin for a prolonged time (Saroha, Yadav, and Sharma 2011). The transdermal patch containing trigonelline (10%)-based standardized fenugreek extract (carbomer-940 and polyethylene glycol) was reported to decrease pain score, post-surgery demand for subcutaneous morphine in comparison to diclofenac dermal patch (1%) in patients of inguinal hernia post-operative pain during a double-blind placebo-controlled clinical study (Ansari et al. 2019). Gradual reduction in pain during 6 h and after 24 h of surgery was reported on patients treated with fenugreek patch as measured by a visual analogue scale (the pain sensation in the range of 0 to 10) with reduced side effects of morphine and no allergic side effects (Ansari et al. 2019).
Drug Delivery and Bioavailability in Short Bowel Syndrome
John K. DiBaise, Carol Rees Parrish, Jon S. Thompson in Short Bowel Syndrome Practical Approach to Management, 2017
The adhesive transdermal drug delivery patch was first approved by the Food and Drug Administration in 1979 for scopolamine used to treat motion sickness [32]. Transdermal patches utilize either a drug reservoir or the drug is impregnated into the fabric of the patch. Upon applying the patch to the skin, the drug diffuses toward the skin tissue based on the concentration gradient. As a result, a second drug reservoir is established in the stratum corneum. As the drug molecules penetrate further into the skin, they are absorbed into the local capillary vasculature and, eventually, into the systemic circulation [33]. This reservoir-mediated absorption process results in a drug absorption rate that is gradual and slow. Therefore, the onset of action of drugs administered as a transdermal patch is delayed. It is not unusual to take up to three patch applications to achieve steady-state plasma drug concentration. Therefore, transdermal patches are generally used for maintenance therapy and have no role in the acute management of symptoms. For example, a clonidine patch can be used as maintenance therapy for hypertension in patients with SBS; however, oral clonidine tablets should be used for immediate control of blood pressure [4]. Because a drug reservoir is formed in the stratum corneum, the drug may continue to have clinical effect for hours or even days after the patch is removed from the skin.
Preclinical and Clinical Safety Assessment of Transdermal and Topical Dermatological Products
Tapash K. Ghosh in Dermal Drug Delivery, 2020
Since 1979, after the U.S. FDA approved the first transdermal patch, there has been successful marketing of numerous transdermal drug delivery systems. Transdermal patches have advantages over oral medications including reduction of first-pass drug-degradation effects, reduction in adverse effects and convenient painless medication administration. Efforts have been made to improve transdermal transport with chemical enhancers, use of electric fields (iontophoresis and electroporation) and ultrasound. However, many limitations exist in the development of transdermal delivery systems, which partly account for the limited number of products marketed over the last 30 years. The assessment of the safety of transdermal and topical dermatologic products is often a long and incompletely developed process, but on the basis of three decades of experience, manageable.
Mathematical modelling of drug-diffusion from multi-layered capsules/tablets and other drug delivery devices
Published in Computer Methods in Biomechanics and Biomedical Engineering, 2022
Saqib Mubarak, M. A. Khanday
Transdermal drug delivery provides an adequate suitable route for oral drug delivery having a large number of benefits over other drug delivery routes. A typical transdermal patch is composed of an adhesive matrix which contains the drug in-between a backing layer and release liner. Examples include nicotine patches which deliver a constant dose of nicotine across the skin that helps to relieve the symptoms associated with tobacco withdrawal, scopolamine for motion sickness, testosterone and oestrogen for replacement therapy, nitroglycerin for angina pectoris, fentanyl as analgesia and clonidine for hypertension. Therefore in this case, the domain consists of a two-layered transdermal patch and various layers of the skin (target tissue), mentioned in Table 3. Thus in this framework, there is an aggregate of nine layers (two layers of the transdermal patch and seven layers of the dermal region). Hence, taking n = 9, Eqs. (21) and (22) are simulated using the physiological values of various parameters given in Tables 3 and 4 with the help of Wolfram MATHEMATICA software, to obtain the concentration and diffusion profiles in the corresponding layers. The model simulations are presented graphically in Figures 11 and 12.
Microneedle system: a modulated approach for penetration enhancement
Published in Drug Development and Industrial Pharmacy, 2021
Nirupma Khare, Pravin Shende
The topical drug delivery system is most preferred over parenteral and oral routes of administration because they bypass the first-pass metabolism, offers ease of application, and avoids the pain caused by the needle (as needles penetrate till the dermal layer of skin consisting of nerve endings) and trypanophobia (fear of needles). Transdermal patches are considered as an alternative to topical formulations as the application is easier but permeability across the skin acts as a barrier for the systemic administration of drugs. However, many drugs such as anti-cancer drugs, genes, proteins, and peptides are not administered via the transdermal route because of the physicochemical properties of the active and nature of stratum corneum [1,2]. The suitability of drugs for transdermal delivery is influenced by the following factors: (1) nonirritant to skin and not stimulate a reaction, (2) have a molecular weight less than 500 Da, (3) potent drugs with a systemic dose of less than or equal to 20 mg, (4) lipophilic with the log P range 1–3, (5) have a melting point less than 200 °C, (6) have less than or equal to 2 hydrogen bonding groups [3].
Modeling percutaneous absorption for successful drug discovery and development
Published in Expert Opinion on Drug Discovery, 2020
Hanumanth Srikanth Cheruvu, Xin Liu, Jeffrey E. Grice, Michael S. Roberts
Drugs are applied to the skin to generate either a local or a systemic effect. Topical delivery systems are usually designed to deliver the active ingredient to local tissue and are mainly used as protectives, cosmetics, pain relievers or to treat dermatological disease, while transdermal delivery systems are designed to achieve systemic absorption of the drug (Figure 2). Most topical products are semi-solid formulations (creams, ointments, gels, and pastes), liquid dispersions (solutions, suspensions, emulsions, and lotions) or solid powders. Transdermal products are mainly formulated as transdermal patches for controlled delivery of drugs such as nitroglycerin, clonidine, nicotine, and scopolamine. Three drivers have been recognized for a drug candidate to be considered for topical or transdermal applications [1]. Firstly, does the drug candidate have the appropriate physicochemical properties to be absorbed across the skin or to be retained in the skin? Secondly, does the new drug have sufficient potency and a sufficiently low clearance to be active at the site of action? Lastly, is there any significant advantage of topical or transdermal delivery compared to other routes of administration?
Related Knowledge Centers
- Adhesive
- Motion Sickness
- Nicotine
- Nicotine Patch
- Circulatory System
- Skin
- Scopolamine
- Medication
- Dose
- Microneedle Drug Delivery