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Open accessJournal ArticleDOI: 10.1007/S40005-021-00512-4

Microneedle for transdermal drug delivery: current trends and fabrication

04 Mar 2021-Journal of Pharmaceutical Investigation (Springer Singapore)-Vol. 51, Iss: 5, pp 1-15
Abstract: Transdermal delivery has the advantage of bypassing the first-pass effect and allowing sustained release of the drug. However, the drug delivery is limited owing to the barrier created by the stratum corneum. Microneedles are a transdermal drug delivery system that is painless, less invasive, and easy to self-administer, with a high drug bioavailability. The dose, delivery rate, and efficacy of the drugs can be controlled by the microneedle design and drug formulations. This review introduces the types of microneedles and their design, materials used for fabrication, and manufacturing methods. Additionally, recent biological applications and clinical trials are introduced. With advancements made in formulation technologies, the drug-loading capability of microneedles can be improved. 3D printing and digital technology contribute to the improvement of microneedle fabrication technology. However, regulations regarding the manufacture of microneedle products should be established as soon as possible to promote commercialization.

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Topics: Transdermal (58%), Drug delivery (55%)
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12 results found


Open accessJournal ArticleDOI: 10.1186/S40824-021-00226-6
Abstract: Various non-invasive administrations have recently emerged as an alternative to conventional needle injections. A transdermal drug delivery system (TDDS) represents the most attractive method among these because of its low rejection rate, excellent ease of administration, and superb convenience and persistence among patients. TDDS could be applicable in not only pharmaceuticals but also in the skin care industry, including cosmetics. Because this method mainly involves local administration, it can prevent local buildup in drug concentration and nonspecific delivery to tissues not targeted by the drug. However, the physicochemical properties of the skin translate to multiple obstacles and restrictions in transdermal delivery, with numerous investigations conducted to overcome these bottlenecks. In this review, we describe the different types of available TDDS methods, along with a critical discussion of the specific advantages and disadvantages, characterization methods, and potential of each method. Progress in research on these alternative methods has established the high efficiency inherent to TDDS, which is expected to find applications in a wide range of fields.

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Topics: Transdermal (55%)

4 Citations


Open accessJournal ArticleDOI: 10.53049/TJOPAM.2021.V001I03.010
31 Aug 2021-
Abstract: Because of the limitations of the oral drug delivery system, as well as the discomfort associated with the usage of needles in the case of injections, drug delivery research has shifted significantly toward the transdermal route of administration. Topical creams, gels, and transdermal patches are the most often utilised means of transdermal administration of drugs. Since the stratum corneum layer of the skin acts as a barrier to a drug molecule, the effect of the majority of therapeutic agents is limited. As a result, only a small number of molecules are able to reach the site of action. A new type of delivery method, known as microneedles, is being developed to improve the distribution of drugs through this route while also overcoming the various issues associated with existing formulations. Non-invasive and painless feature of microneedles have making them ideal for self-administration. This review describes various type of microneedles and their design, fabrication methodology, various materials used in fabrication of microneedles, drug release mechanism from the microneedles, evaluation parameters, it’s biological application, update about recent clinical studies and in last, challenges and future perspective of microneedles as drug delivery system.

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Topics: Transdermal (62%), Transdermal route (58%), Drug delivery (55%)

3 Citations


Open accessJournal ArticleDOI: 10.1039/D1AY00954K
05 Aug 2021-Analytical Methods
Abstract: The fast-advancing progress in the research of nanomedicine and microneedle applications in the past two decades has suggested that the combination of the two concepts could help to overcome some of the challenges we are facing in healthcare. They include poor patient compliance with medication and the lack of appropriate administration forms that enable the optimal dose to reach the target site. Nanoparticles as drug vesicles can protect their cargo and deliver it to the target site, while evading the body's defence mechanisms. Unfortunately, despite intense research on nanomedicine in the past 20 years, we still haven't answered some crucial questions, e.g. about their colloidal stability in solution and their optimal formulation, which makes the translation of this exciting technology from the lab bench to a viable product difficult. Dissolvable microneedles could be an effective way to maintain and stabilise nano-sized formulations, whilst enhancing the ability of nanoparticles to penetrate the stratum corneum barrier. Both concepts have been individually investigated fairly well and many analytical techniques for tracking the fate of nanomaterials with their precious cargo, both in vitro and in vivo, have been established. Yet, to the best of our knowledge, a comprehensive overview of the analytical tools encompassing the concepts of microneedles and nanoparticles with specific and successful examples is missing. In this review, we have attempted to briefly analyse the challenges associated with nanomedicine itself, but crucially we provide an easy-to-navigate scheme of methods, suitable for characterisation and imaging the physico-chemical properties of the material matrix.

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2 Citations


Journal ArticleDOI: 10.1016/J.ADDR.2021.113957
Abstract: Non-oral long-acting drug delivery systems (LADDS) encompass a range of technologies for precisely delivering drug molecules into target tissues either through the systemic circulation or via localized injections for treating chronic diseases like diabetes, cancer, and brain disorders as well as for age-related eye diseases. LADDS have been shown to prolong drug release from 24 h up to 3 years depending on characteristics of the drug and delivery system. LADDS can offer potentially safer, more effective, and patient friendly treatment options compared to more invasive modes of drug administration such as repeated injections or minor surgical intervention. Whilst there is no single technology or definition that can comprehensively embrace LADDS; for the purposes of this review, these systems include solid implants, inserts, transdermal patches, wafers and in situ forming delivery systems. This review covers common chronic illnesses, where candidate drugs have been incorporated into LADDS, examples of marketed long-acting pharmaceuticals, as well as newly emerging technologies, used in the fabrication of LADDS.

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Topics: Drug delivery (55%), Transdermal (52%)

1 Citations


Journal ArticleDOI: 10.1016/J.IJPHARM.2021.121204
Abstract: Malaria caused by various types of Plasmodium has become a global health problem. One of the drugs used as the first line of malaria therapy is primaquine (PMQ). PMQ is generally administered through the oral route. However, the use of PMQ orally could potentially cause some side effects and undergo the first-pass metabolism in the liver, reducing its effectiveness. Therefore, it is necessary to develop another drug administration route to avoid this effect. In this study, for the first time, PMQ was formulated into a transdermal patch for transdermal delivery, combined with solid microneedles, Dermaroller®. Following several optimizations, HPMC and glycerin were used as the main polymer and plasticizer, respectively. Specifically, the concentration of PEG 400 as a permeation enhancer was also optimized. The transdermal patches were evaluated for weight uniformity, thickness, surface pH, folding endurance, moisture content, moisture absorption ability, bioadhesive evaluation, and drug content recovery. PMQ release and permeation were also investigated through in vitro and ex vivo tests on rats’ skin tissue. Importantly, the safety of the transdermal patch was also evaluated through in vitro hemolytic and in vivo irritation tests which were confirmed by histopathological examinations. The results showed that all formulations showed desired physical and bioadhesive properties with a folding endurance of >300 folds. The results exhibited that 31.31 ± 5.25% and 22.55 ± 4.35% of primaquine were released from transdermal patches following the in vitro and the ex vivo permeation studies. Combined with Dermaroller®, the ex vivo permeation study showed an improved permeation profile with 45.89 ± 5.00% of primaquine permeated after 24 h with a zero-order kinetic during the first 8 h. Hemolysis percentage was found to be

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Topics: Transdermal (69%), Transdermal patch (62%)

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100 results found


Open accessJournal ArticleDOI: 10.1038/NBT.1504
Mark R. Prausnitz1, Robert Langer2Institutions (2)
Abstract: Transdermal drug delivery has made an important contribution to medical practice, but has yet to fully achieve its potential as an alternative to oral delivery and hypodermic injections. First-generation transdermal delivery systems have continued their steady increase in clinical use for delivery of small, lipophilic, low-dose drugs. Second-generation delivery systems using chemical enhancers, noncavitational ultrasound and iontophoresis have also resulted in clinical products; the ability of iontophoresis to control delivery rates in real time provides added functionality. Third-generation delivery systems target their effects to skin's barrier layer of stratum corneum using microneedles, thermal ablation, microdermabrasion, electroporation and cavitational ultrasound. Microneedles and thermal ablation are currently progressing through clinical trials for delivery of macromolecules and vaccines, such as insulin, parathyroid hormone and influenza vaccine. Using these novel second- and third-generation enhancement strategies, transdermal delivery is poised to significantly increase its impact on medicine.

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Topics: Transdermal (67%), Targeted drug delivery (57%), Transdermal route (57%) ... show more

2,192 Citations


Open accessJournal ArticleDOI: 10.1016/J.BIOMATERIALS.2010.04.050
01 Aug 2010-Biomaterials
Abstract: Stereolithography is a solid freeform technique (SFF) that was introduced in the late 1980s. Although many other techniques have been developed since then, stereolithography remains one of the most powerful and versatile of all SFF techniques. It has the highest fabrication accuracy and an increasing number of materials that can be processed is becoming available. In this paper we discuss the characteristic features of the stereolithography technique and compare it to other SFF techniques. The biomedical applications of stereolithography are reviewed, as well as the biodegradable resin materials that have been developed for use with stereolithography. Finally, an overview of the application of stereolithography in preparing porous structures for tissue engineering is given.

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Topics: Stereolithography (61%)

1,418 Citations


Journal ArticleDOI: 10.1021/JS980042+
Abstract: Although modern biotechnology has produced extremely sophisticated and potent drugs, many of these compounds cannot be effectively delivered using current drug delivery techniques (e.g., pills and injections). Transdermal delivery is an attractive alternative, but it is limited by the extremely low permeability of skin. Because the primary barrier to transport is located in the upper 10-15 micron of skin and nerves are found only in deeper tissue, we used a reactive ion etching microfabrication technique to make arrays of microneedles long enough to cross the permeability barrier but not so long that they stimulate nerves, thereby potentially causing no pain. These microneedle arrays could be easily inserted into skin without breaking and were shown to increase permeability of human skin in vitro to a model drug, calcein, by up to 4 orders of magnitude. Limited tests on human subjects indicated that microneedles were reported as painless. This paper describes the first published study on the use of microfabricated microneedles to enhance drug delivery across skin.

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Topics: Transdermal (55%), Drug delivery (51%)

1,057 Citations


Open accessJournal ArticleDOI: 10.1016/J.ADDR.2012.04.005
Abstract: Microneedles were first conceptualized for drug delivery many decades ago, but only became the subject of significant research starting in the mid-1990's when microfabrication technology enabled their manufacture as (i) solid microneedles for skin pretreatment to increase skin permeability, (ii) microneedles coated with drug that dissolves off in the skin, (iii) polymer microneedles that encapsulate drug and fully dissolve in the skin and (iv) hollow microneedles for drug infusion into the skin. As shown in more than 350 papers now published in the field, microneedles have been used to deliver a broad range of different low molecular weight drugs, biotherapeutics and vaccines, including published human studies with a number of small-molecule and protein drugs and vaccines. Influenza vaccination using a hollow microneedle is in widespread clinical use and a number of solid microneedle products are sold for cosmetic purposes. In addition to applications in the skin, microneedles have also been adapted for delivery of bioactives into the eye and into cells. Successful application of microneedles depends on device function that facilitates microneedle insertion and possible infusion into skin, skin recovery after microneedle removal, and drug stability during manufacturing, storage and delivery, and on patient outcomes, including lack of pain, skin irritation and skin infection, in addition to drug efficacy and safety. Building off a strong technology base and multiple demonstrations of successful drug delivery, microneedles are poised to advance further into clinical practice to enable better pharmaceutical therapies, vaccination and other applications.

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1,009 Citations


Open accessJournal ArticleDOI: 10.1073/PNAS.2331316100
Abstract: Arrays of micrometer-scale needles could be used to deliver drugs, proteins, and particles across skin in a minimally invasive manner. We therefore developed microfabrication techniques for silicon, metal, and biodegradable polymer microneedle arrays having solid and hollow bores with tapered and beveled tips and feature sizes from 1 to 1,000 μm. When solid microneedles were used, skin permeability was increased in vitro by orders of magnitude for macromolecules and particles up to 50 nm in radius. Intracellular delivery of molecules into viable cells was also achieved with high efficiency. Hollow microneedles permitted flow of microliter quantities into skin in vivo, including microinjection of insulin to reduce blood glucose levels in diabetic rats.

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731 Citations