Dissolvable and Coated Microneedle Arrays: Design, Fabrication, Materials and Administration Methods
Boris Stoeber, Raja K Sivamani, Howard I. Maibach in Microneedling in Clinical Practice, 2020
Although many advantages of transdermal and cutaneous (i.e., intradermal) delivery have been well recognized, they have yet to be fully exploited. Transdermal and cutaneous routes present their own challenges: delivering drugs through these routes requires overcoming the physical barrier imposed by the stratum corneum (SC), the top layer of the skin [5]. Without a physical breach or chemical penetration enhancers, only small molecules (<500 Da molecular weight) can penetrate the SC [6–8]. This puts significant limits on the types of proteins, peptides, and genetic materials (i.e., polyplexes and recombinant viral vectors) that can be directly delivered to or through the skin, thereby hindering the use of transdermal and intradermal routes for a majority of vaccines and therapeutics without the use of specifically designed delivery systems [9, 10].
Androgen production over the female life span
Barry G. Wren in Progress in the Management of the Menopause, 2020
We have therefore investigated a matrix transdermal delivery system in an attempt to achieve more physiological and stable levels in women. Transdermal delivery of drugs offers several advantages including rapid perfusion through the skin, painless delivery, increased compliance and avoidance of the first-pass hepatic metabolism. We have examined (Buckler, Robertson and Wu, unpublished data) the pharmacokinetics of a matrix transdermal system (TDS) for testosterone using various estimated daily T delivery rates aiming to produce stable physiological levels in women. As can be seen (Figures 5 and 6) this delivery system produced T levels which may be appropriate for use in women. The TDS was well tolerated by all subjects with no evidence of any local skin reaction even with repeated applications.
Recent Cannabinoid Delivery Systems
Betty Wedman-St Louis in Cannabis as Medicine, 2019
Transdermal administration delivers drugs through the skin via patches or other delivery systems. Although comparable to oral-dosage forms in term of efficacy, transdermal patches provide numerous advantages. Transdermal administration avoids the first-pass metabolism effect that is associated with the oral route and thus improves drug bioavailability. Furthermore, transdermal administration allows a steady infusion of a drug to be delivered over a prolonged period of time, while also minimizing the adverse effects of higher drug peak concentrations, which can improve patient adherence. Topical administration is potentially ideal for localized symptoms, such as those found in dermatological conditions and arthritis but also in peripheral neuropathic pain for which capsaicin patches have been proposed as a second line treatment after high quality of evidence was provided [91]. However, there are some disadvantages to consider, such as the possibility of local irritation and the low skin penetration of drugs with a hydrophilic structure. Indeed, drugs that are slightly lipophilic (logP 1–4) have a molecular mass of less than 500 Da and that show efficacy at low dosage (less than 10 mg/day for transdermal administration) are ideal for administration via this route. Enhancers may also be added to transdermal formulations to increase the penetration of permeants by disrupting the structure of the skin’s outer layer, i.e. the stratum corneum, and increasing penetrant solubility.
Lipidic cubic-phase leflunomide nanoparticles (cubosomes) as a potential tool for breast cancer management
Published in Drug Delivery, 2022
Mariam Zewail, Passent M. E. Gaafar, Mai M. Ali, Haidy Abbas
Transdermal drug delivery is a noninvasive route for systemic delivery of drugs across the skin layers. It has several merits compared to oral or parenteral routes as it can overcome gastrointestinal barriers, first pass metabolism in addition to its acceptability for patients (Nasr et al., 2020). Nanotechnology has numerous applications in diagnosing, monitoring, imaging, and delivering drugs to the tumor site (Vieira & Gamarra, 2016; Jain et al., 2020). Nanocarriers like polymeric nanoparticles (Jain et al., 2013; Li, Sun et al., 2015), liposomes (Ahmad et al., 2016), micelles (Guo et al., 2019), microspheres (Pal et al., 2019), dendrimers (Gupta et al., 2010; Chittasupho et al., 2017), solid lipid nanoparticles (Fontana et al., 2005; Acevedo-Morantes et al., 2013) and nanostructured lipid carriers (Sun et al., 2014) have been investigated over the past decade to increase the therapeutic efficacy of chemotherapeutic agents delivery to the targeted tumor site (Jain et al., 2020).
Long-acting HIV pre-exposure prophylaxis (PrEP) approaches: recent advances, emerging technologies, and development challenges
Published in Expert Opinion on Drug Delivery, 2022
Vivek Agrahari, Sharon M. Anderson, M. Melissa Peet, Andrew P. Wong, Onkar N. Singh, Gustavo F. Doncel, Meredith R. Clark
Drug delivery using transdermal patches is beneficial to potential users, since these can be painlessly self-applied with no need for specialized disposal [123–125]. CONRAD, in collaboration with Mercer University, developed a silicone-based suspension patch for sustained weekly delivery of TAF free base [123]. The patch was tested in female hairless rats and achieved the target PK profile, duration, and safety for a once-weekly TAF delivery for HIV prevention or treatment [126]. Eliminating the need for wearing a patch for a prolonged period of time and to provide a LA drug delivery, the recently developed microarray patches (MAP) are minimally invasive devices that are applied and removed minutes later, consisting of microscopic projections to penetrate the skin’s upper layers or mucosal tissues to administer the drug [125,127,128]. Donnelly et al. in collaboration with PATH, developed a dissolving MAP containing LA nanosuspension of RPV [129]. Most recently, they have also developed a bilayer MAP loaded with CAB [130] and a dissolvable and implantable MAP loaded with TAF [131] for long-term HIV PrEP (Figure 3c). CONRAD in partnership with the University of Connecticut is further developing this technology for the delivery of bnAbs (manuscript submitted).
Fentanyl use disorder characterized by unprescribed use of transdermal patches: a case report
Published in Journal of Addictive Diseases, 2022
Cavid Guliyev, Zehra Olcay Tuna, Kültegin Ögel
Fentanyl is a pure mu receptor agonist that crosses the blood–brain barrier rapidly. Its analgesic effect is 75–100 times higher than that of morphine.1 The routes of administration for prescribed use include oral, intravenous, epidural, transdermal, intranasal, and transmucosal routes. Transdermal fentanyl patch (TFP) has been widely used as an effective analgesic since 1990.2 TFP has several clinical advantages, such as long-acting analgesic effect and low incidence of undesirable side effects compared to morphine. Owing to such features, the use of TFP has been accepted as a noninvasive method for pain relief.3 Because of its low molecular weight and lipophilic properties, fentanyl is easily absorbed through skin.4 TFPs are available in doses of 25, 50, 75, and 100 mcg/hour. The effect of fentanyl lasts for up to 72 hours when used as transdermal patches.2 Compared to other forms, TFPs have a reduced possibility of misuse due to the fact that TFPs release the drug in a sustained and long-acting manner with a stable serum concentration.5 In addition, it is accepted that the risk of developing tolerance and use disorder is minimal because it rarely causes euphoria.6
Related Knowledge Centers
- Epidermis
- Nanomedicine
- Transcellular Transport
- Transdermal Patch
- Dermis
- Stratum Corneum
- Route of Administration
- Collagen Induction Therapy
- Vaccine
- Invasomes