Use Of Transdermal Delivery Research Articles

Designing Polyelectrolyte Microneedles Based on Borylated Poly(β-aminoester) Polymers To Enhance Transdermal pH-Controlled Delivery of Nucleic Acids.

The use of transdermal delivery for nucleic acid administration is an interesting approach to overcoming limitations of systemic administration routes, such as first-pass effects, the painful needle injection, or their poor biodistribution. Thus, the use of a microneedle-based patch could represent a turning point for nucleic acid delivery, thanks to the possibility of self-administration of the actives in a painless and easy procedure. However, the design of transdermal systems with a higher degree of precision release is a clear need that has not been fully resolved. Committed to tackling this challenge, we present here a microneedle patch that involves a smart delivery system supported by the well-established ability of boronic acid to interact with carbohydrates in a pH-dependent manner. This system builds up a multilayer structure over a solid microneedle platform whose surface has been modified to immobilize glucosamine units that are able to interact with an oligopeptide-end terminated poly(β-aminoester) that presents a 4-carboxy-3-fluorophenylboronic acid (Bor-pBAE). Thus, sequential layers of the Bor-pBAE and plasmid DNA have been assembled, thanks to the ability of the polymer to interact with the nucleic acid at a basic pH and then gradually release the plasmid under two different conditions of pH (the physiological pH = 7.4 and the acidic pH = 5.1). We set up the design and implementation of this first proof of concept while demonstrating microneedles' safety and functionality. Additionally, we have shown the efficacy of the construct to express the encoded genes in model cell lines. In conclusion, we have established the basis to confirm that this generation of borylated poly(β-aminoesters) holds great promise as a transdermal local nucleic acid delivery system.

Recent Update on Nanoemulsion Impregnated Hydrogel: a Gleam into the Revolutionary Strategy for Diffusion-Controlled Delivery of Therapeutics.

Since earlier times, dermatological remedies have been utilized to treat diseases associated with pain, irritation, and skin conditions. Compared to other routes of drug delivery, topical delivery of drugs offers several benefits. Scientists are investigating different alterations in dosage forms in addition to existing topical formulations such as ointments, gels, creams, lotions, and ointments to significantly improve the permeation of drugs and enhance the pharmacological efficacy of medications that are poorly absorbed via the skin. Conventional formulations have a plethora of problems viz. poor absorption, no target specificity, low spreadability, and inadequate bioavailability which leads the researchers toward developing novel formulations like nanoemulsions. The nanoemulsion can enhance the gradient in concentration and thermodynamic movement toward the epidermis and enhance the penetration of its constituents. However, due to its difficult application, nanoemulsion's lower viscosity limited its use in transdermal delivery. Thus, the development of nanoemulsion-based hydrogels has shown to be a successful strategy for removing obstacles from existing drug formulations. The simple application, expedient spreadability, non-stickiness, safety, and effectiveness of nanoemulsion-based hydrogel have led to substantial growth in their research in recent years. This review gives a brief idea about the prevalence of skin diseases, skin as an obstacle for drug delivery, and recent research insights to combat these obstacles. The work highlights the mechanism of drug release via nanoemulsion, hydrogels, and nanoemulsion-based hydrogels with reference to recent research on hydrophobic and hydrophilic drugs.

AN OVERVIEW: RECENT DEVELOPMENT IN TRANSDERMAL DRUG DELIVERY

The transdermal drug delivery system is an alternative method of administration of drugs. Most of the drugs are delivered by conventional oral, topical, intravenous, and intramuscular methods and are is of limited efficiency. However, now the clinical use of transdermal delivery is limited because of stratum cornea of the skin act as an effective barrier that limits the permeation of drugs through the skin. To overcome this disadvantage, there are Recent developments in transdermal drug delivery, such as the usage of nanoparticles i.e., liposomes, niosomes, transferosomes, ethosomes, nanoemulsion, virosomes, phytosomes, dendrimers, proniosomes, microneedles, and separable microneedles. This nanoparticulate transdermal drug delivery exhibits great potential to ensure drug permeation through the skin. They are very tiny carriers to detect by the immune system and further, they can be delivering the drug to the targeted site and also have the ability to deliver both hydrophilic and hydrophobic drugs by reducing the complexity. Nanoparticles are made of different materials and they’re very different in structure and chemical properties are discussed in this review article.

ANTI-NEOPLASTIC TRANSDERMAL PATCHES: A NOVEL APPROACH FOR TARGETED DRUG DELIVERY USING NANOCARRIERS IN CANCER THERAPY

Innovative Nano-carrier-based transdermal patches, a wonder of advanced technologies, have received overwhelming endorsement in medicinal applications primarily in the provision of anti-neoplastic drugs. The purpose of this study was to review the limitations of conventional therapeutic initiatives namely chemotherapy, having several adverse effects, including significant inflammation, toxicity, and discomfort. Antineoplastic transdermal patches can be used as a prophylactic treatment method to treat a variety of cancers through the skin. Novel transdermal methods and Nanocarrier formulations have evolved to resolve the skin constraints and delivering the active drug to the underlying tissue of the skin enabling access to the systemic absorption of drugs and eventually get within tumour cells by approaching different targeting mechanisms. The transdermal administration of antineoplastic drugs is a promising alternative for boosting site-specific application, minimizing adverse effects, hepatic first-pass metabolism and promoting therapeutic value. Furthermore, the utilization of nanocarriers serves as a permeation enhancer to broaden the spectrum of medicines accessible for transdermal administration that has emerged as a viable and intriguing option. This review examines the benefits of transdermal delivery for anti-neoplastic drugs to ensure a good insight into their effectiveness in terms of modern clinical demands, to present a highlighted overview of transdermal drug delivery, and seeks to better comprehend the nano-formulations employed in transdermal drug delivery system (TDDS). Conclusively, reflecting the framework for future research and promoting the chemotherapeutic use of transdermal delivery over conventional dosage forms.

Microemulsion-based Transdermal Drug Delivery System incorporating Levofloxacin hemihydrate for skin Infections

Due to poor bioavailability through the gastrointestinal tract, the oral delivery of drugs has been a challenge for pharmacologists. The study investigated an appropriate microemulsion system suitable for transdermal use. A microemulsion system containing tween 20/1-propanol/water/clove oil was developed for use in transdermal delivery of Levofloxacin hemihydrate. The system was investigated by constructing a pseudo-ternary phase diagram via water-titration method. The stability of water-in-oil microemulsion system was characterized by pH, refractive index measurements, UV-Vis. spectroscopy and measurement of partition coefficient and particle size. This study demonstrated that Levofloxacin hemihydrate can be successfully incorporated into a water-in-oil (w/o) microemulsion system consisting of tween20 (surfactant) /1-propanol (co-surfactant) /water and clove oil. This microemulsion system can be modified for use as an ointment to treat skin infections by both gram-positive and gram-negative bacteria as well as anaerobes.

Plant plasma membrane vesicles interaction with keratinocytes reveals their potential as carriers

During the last few years, membrane vesicles (as exovesicles) have emerged as potential nanocarriers for therapeutic applications. They are receiving attention due to their proteo-lipid nature, size, biocompatibility and biodegradability. In this work, we investigated the potential use of isolated root plasma membrane vesicles from broccoli plants as nanocarriers. For that, the entrapment efficiency and integrity of the vesicles were determined. Also, the delivery of keratinocytes and penetrability through skin were studied. The results show that the broccoli vesicles had high stability, in relation to their proteins, and high entrapment efficiency. Also, the interaction between the vesicles and keratinocytes was proven by the delivery of an encapsulated fluorescent product into cells and by the detection of plant proteins in the keratinocyte plasma membrane, showing the interactions between the membranes of two species of distinct biological kingdoms. Therefore, these results, together with the capacity of brassica vesicles to cross the skin layers, detected by fluorescent penetration, enable us to propose a type of nanocarrier obtained from natural plant membranes for use in transdermal delivery.

Deep Eutectic Solvent-Induced Structural Transition of Microemulsions Explored with Small-Angle X-ray Scattering

Microemulsions (MEs) containing deep eutectic solvents (DESs) and water in the inner phase for use in transdermal delivery of poorly soluble drugs were prepared using a mixture of polyoxyethylene sorbitan monooleate (Tween-80) and sorbitan laurate (Span-20) as surfactants. We investigated the effects of the ratios of surfactant (Tween-80/Span-20) and solvents (DES components/water) on the ME structure determined by the analysis of small-angle X-ray scattering profiles with the core-corona model. Tween-80 with an unsaturated long alkyl chain induced a structural transition of MEs from a sphere to a cylinder. DESs caused the aggregation of surfactants due to the solvophobic interactions between DESs and the alkyl chains of surfactants. Transmittance electron microscopy images of MEs indicated the presence of aggregates of the dispersed ME particles with each shape.

Accuracy and feasibility of piezoelectric inkjet coating technology for applications in microneedle-based transdermal delivery

Coated microneedles have shown immense promise for use in transdermal delivery and diagnostics, due to their ability to painlessly breach the skin's outermost stratum corneum layer and interact with the epidermal layers immediately beneath. In this work, we use an off-the-shelf piezoelectric dispensing system to demonstrate the feasibility of depositing material directly on to steeply-sloping microneedle sidewalls, without the need for specific needle array positioning or material pretreatment. In the first instance, an analysis of deposition accuracy shows that over 95% of dispensed droplets land within 20μm of the target. Through the use of sequential dispense and drying steps, 3.2nL of a model drug formulation has been deposited onto both silicon and polymeric microneedles with highly sloped (71°) sidewalls; these are the steepest surfaces that have been coated to date. Finally, preliminary ex-vivo skin studies have been performed to show that the material may be successfully transferred from the needle to skin. Despite the smooth surfaces, ultrasharp tips and steep sidewalls of these structures, piezoelectric dispense techniques are clearly feasible for microneedle coating and may offer a promising alternative to conventional coating processes.

Quality by design approach to prepare oleoyl alginate derivative and its use in transdermal delivery

The aim of this study is to prepare an optimized surface active modified polysaccharide gel of oleoyl alginate using response surface methodology as well as to study its potential use in drug skin delivery as a safe alternative to skin penetration enhancers. An optimized oleoyl alginate material was obtained using response surface methodology in terms of three different responses, i.e. degree of substitution, viscosity and surface tension. The resultant optimized oleoyl alginates were further studied concerning particle size, surface roughness and particle aggregation concentration measurements. Franz diffusion cell method was used to monitor skin permeation of ibuprofen lysinate over 6-h period exposure to excised rabbit skin. The optimized oleoyl alginate based on surface tension showed the highest particle size, the lowest surface tension among other preparations and it has also been used as skin penetration enhancer for ibuprofen lysinate. In this study, a polysaccharide derivative was prepared that enhanced skin penetration ability of the model drug i.e. ibuprofen lysinate.

Nanocarriers for transdermal drug delivery

Nanocarriers for transdermal drug delivery José Juan Escobar-Chávez,1 Roberto Díaz-Torres,2 Isabel Marlen Rodríguez-Cruz,3 Clara Luisa Domínguez-Delgado,4 Rafael Sampere Morales,5 Enrique Ángeles-Anguiano,6 Luz María Melgoza-Contreras71Sistemas Transdérmicos y Materiales Nanoestructurados, 2Toxicología y Genética, Universidad Nacional Autónoma de México, Cuautitlán Izcalli, México; 3Unidad de Enseñanza e Investigación, Hospital Regional de Alta Especialidad de Zumpango, Zumpango, México; 4Departamento de Ingeniería y Tecnología, 5Departamento de Ciencias Químicas, 6Laboratorio de Química Medicinal, Universidad Nacional Autónoma de México, Cuautitlán Izcalli, México; 7Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco, México City, MéxicoAbstract: Transdermal drug delivery offers an attractive alternative to the conventional drug-delivery methods of oral administration and injection. Apart from the convenience and noninvasiveness, the skin also provides a “reservoir” that sustains delivery over a period of days. It offers multiple sites to avoid local irritation and toxicity, yet it can also offer the option of concentrating drugs at local areas to avoid undesirable systemic effects. However, at present, the clinical use of transdermal delivery is limited by the fact that very few drugs can be delivered transdermally at a viable rate. This difficulty is because the stratum corneum of skin acts as an efficient barrier that limits penetration of drugs through the skin, and few noninvasive methods are known to significantly enhance the penetration of this barrier. In order to increase the range of drugs available for transdermal delivery, the use of nanocarriers has emerged as an interesting and valuable alternative for delivering lipophilic and hydrophilic drugs throughout the stratum corneum with the possibility of having a local or systemic effect for the treatment of many different diseases. These nanocarriers (nanoparticles, ethosomes, dendrimers, liposomes, etc) can be made of a lot of different materials, and they are very different in structure and chemical nature. They are too small to be detected by the immune system, and furthermore they can deliver the drug in the target organ using lower drug doses in order to reduce side effects.Keywords: skin, transdermal drug delivery, transdermal nanocarriers, nanoparticles, dendrimers, liposomes, nanoemulsions, transfersomes

Transdermal drug delivery in pain management

Transdermal drug delivery is defined as the non-invasive delivery of medications through the skin surface. The use of analgesics as a ‘pain relief patch’ is gaining popularity. When applied to the skin, these patches can deliver an analgesic drug at a predetermined rate across the dermis to achieve either a local or systemic effect. Transdermal delivery of medications is not a new concept. The use of transdermal delivery of homemade medicinal preparations dates to the early 20th century. Mustard plasters were used for severe chest congestion. The Belladonna Plaster, containing 0.25% of Belladonna alkaloid, had a place in the US pharmacopeia as a transdermal analgesic. The success of nicotine patches nearly two decades ago revolutionized the use of transdermal drug delivery. Over the last decade, an increasing number of analgesic drugs have become available as transdermal patches. Patches offer advantages over conventional parenteral or oral routes. They ensure controlled absorption and more uniform plasma drug concentrations. Bioavailability is improved by avoiding first-pass hepatic metabolism and enzymatic or pH-associated deactivation. Delivery of the drug is via a simple and painless application. There is increased flexibility in terminating drug administration by patch removal. Patient compliance is improved as patches are simple, non-invasive, and convenient. Clear labelling ensures rapid identification of medication. There are, however, some limitations to transdermal drug delivery. First, there may be local irritation or sensitization of the skin at the site of patch application. Secondly, not all drugs are suitable for transdermal delivery. Thirdly, this modality is not suitable for shocked patients as decreased peripheral blood flow leads to unreliable transdermal absorption. Finally, in comparison with other routes of drug delivery, the transdermal route is relatively more expensive.

Preparation of Organic Nanoparticles Using Microemulsions: Their Potential Use in Transdermal Delivery

Preparation of Organic Nanoparticles Using Microemulsions: Their Potential Use in Transdermal Delivery

Preparation of Organic Nanoparticles Using Microemulsions: Their Potential Use in Transdermal Delivery

Organic nanoparticles of cholesterol and retinol have been synthesized in various AOT (Aerosol OT; sodium bis(2-ethylhexyl) sulfosuccinate)/heptane/water microemulsions by direct precipitation of the active principle in the aqueous cores. The nanoparticles are observed by transmission electron microscopy (TEM) using the adsorption of a contrasting agent, such as iodine vapor. The size of the nanoparticles can be influenced, in principle, by the concentration of the organic molecules and the diameter of the water cores, which is related to the ratio R=[H2O]/[surfactant]. The particles remain stable for several months. The average diameter of the cholesterol nanoparticles varies between 3.0 and 7.0 nm, while that of retinol varies between 4.0 and 10 nm. The average size of the cholesterol nanoparticles does not change much either as a function of the ratio R or as a function of the concentration of cholesterol. The constant size of the nanoparticles can be explained by the thermodynamic stabilization of a preferential size of the particles. Chloroform is used to carry the active principle into the aqueous cores. Retinol molecules form J-complexes composed of two or three molecules, as detected by UV-visible spectroscopy.

Release characteristics of anionic drug compounds from liquid crystalline gels: Part II. The effects of ion pairing and buffering on the passive delivery of anionic drugs across non-rate-limiting membranes

This is the second in a series of papers that report on the release and transport of a range of anionic drugs (diclofenac, salicylic acid) from liquid crystalline gels and ultimately on their use in transdermal delivery. The previous paper [Fitzpatrick, D., Corish, J., 2005. Release characteristics of anionic drug compounds from liquid crystalline gels for transdermal delivery. Part I. Passive release across non-rate limiting membranes. Int. J. Pharm. 301, 226–236] investigated passive release profiles across a non-rate-limiting membrane: here we report on the search for a suitable model enhancer (benzyl dimethyldodecyl ammonium bromide) for the transdermal delivery of anionic compounds. The results presented reveal a significant role for ion pairing and for buffering, analogous to those found in the investigations of cationic species (salbutamol) by Nolan, L.M.A., Corish, J., Corrigan, O.I., Fitzpatrick, D., 2003. Iontophoretic and chemical enhancement of drug delivery. Part I. Across artificial membranes. Int. J. Pharm. 12, 41–55. The method of vehicle preparation is also investigated. It is shown that ion pairing of the drug with the enhancer decreases the amount of drug available for transport from the liquid crystalline gels into aqueous receptor media. This decrease is directly related to the ratio of the concentration of drug to that of the enhancer. Buffering the vehicle inhibits the ion-pair formation to some extent. Vehicle preparation was also found to influence the degree of ion-pair association. The inclusion of a similarly charged enhancer (oleic acid) to the drug was found not to impede the diffusion of the drug from the gels.