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OALib Journal期刊

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1. Transdermal drug delivery systems for antihypertensive drugs - A review
R. Panner Selvam,Anoop Kumar Singh,T. Sivakumar
International Journal of Pharmaceutical and Biomedical Research (IJPBR) , 2010,
Abstract: Hypertension is one of the largest deaths causing disease for the mankind. Since it is a chronic disease it necessitates long term treatment. The disadvantages of antihypertensive drugs such as more frequent of administration, extensive first pass metabolism and variable bioavailability, make it is an ideal candidate for transdermal drug delivery systems. This article is dedicated to the review of antihypertensive transdermal patches in the perspective of enhancing the bioavailibity as well as in improving the patient compliance. The various antihypertensive drugs considered in the review includes timolol maleate, nicardipine hydrochloride, captopril, atenolol, metoprolol tartrate, clonidine, indapamide, labetolol, pinacidil, verapamil hydrochloride, nitrendipine, nifedipine, nicorandil, propranolol hydrochloride, diltiazem hydrochloride, amlodipine besilate, carvedilol and lisinopril. Clonidine was the first antihypertensive drug developed in the transdermal form. Currently a number of antihypertensive transdermal patches are introduced in to the pharmaceutical market. Most of the reported methods in the literature employed solvent evaporation method or solvent casting method for the preparation of transdermal patches. Depending on the release required over a period of time, the concentrations of polymer, plasticizer and penetrant were varied.
Design and in vitro evaluation of new drug-in-adhesive formulations of fentanyl transdermal patches
ABASHZADEH, SHARYAR,DORKOOSH, FARID,MEHDIZADEH, AMIR,REZA ROUINI, MOHAMMAD,TOLIATE, TAYEBE
- , 2004,
Abstract: Sa？etak The present research was designed to evaluate different matrix, drug-in-adhesive and reservoir formulations of fentanyl transdermal patches. The target was to design drug-in-adhesive patches (DIAPs); a full factorial design was used. Different types and amounts of liquid, pressure-sensitive adhesives (PSAs) were used and evaluated with respect to drug release and adhesive properties. A very simple but precise method, the simplified peel 180° test, was developed to measure and compare adhesive properties of transdermal patches. The results showed that release kinetics obeyed the square root of time or Higuchi model, indicating the diffusion controlled release mechanism. It was found that the amount of fentanyl needed for each 10 cm2 three-days DIAP should be 3.3 mg. The respective amounts for reservoir and matrix patches were 2.5 and 5 mg. It was concluded that acrylic PSAs showed the best adhesion and release properties
Design, Formulation and Evaluation of Transdermal Drug Delivery System of Budesonide  [PDF]
Updesh B Lade, Yogesh M Amgaonkar, Rupesh V Chikhale, Dinesh M Biyani, Milind J Umekar
Pharmacology & Pharmacy (PP) , 2011, DOI: 10.4236/pp.2011.23029
Abstract: Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells such as basophils, eosinophils, T-helper cells, mast cells, and neutrophils. In the nasal mucosa, nasal reactivity to allergens, and release of inflammatory mediators and proteolytic enzymes. Budesonide is very effective and quikly acting as it is rapidly and almost completely absorbed after oral administration, but has poor systemic availability (about 10%) due to extensive first-pass metabolism in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4.. The major metabolites, 6-β- hydroxybudesonide and 16-α-hydroxyprednisolone have less than 1% of the glucocorticoid activity of unchanged drug with a terminal half-life of about 2 - 4 hours. Polymeric films containing Eudragit RL 100: Eudragit RS: drug (7:3:1, 7: 2:1) and Ethyl cellulose: PVP: drug (7:3:1, 7:2:1) were selected for transdermal administration based on evaluation studies. These polymeric films were prepared by mercury substrate method employing PEG-400 as plasticizer. Two different penetration enhancers Urea and Dimethyl sulphoxide (DMSO) were employed in the study. The patches in each group were uniform in drug content, thickness. In Vitro drug permeation, moisture absorption and WVTR studies were carried out on these test patches. It was found that at all humidity condition the absorption increases which were linear to the moisture absorbed. In PVA and EUDRAGIT RL 100 patches the water vapor transmission rate was found to be higher at 75% RH, RT conditions. Therefore at both % RH, RT condition the PVA and EUDRAGIT RL 100 patches provides the best resistance to water vapor. Therefore, when applied to animals (in further studies) these patches may provide more occlusion to water vapor loss from skin thus making atmosphere beneath the skin more humid that aid in drug permeation.
MICRONEEDLES: NOVEL APPROACH TO TRANDERMAL DRUG DELIVERY SYSTEM
Pawar RG,Pawar SD,Gadhave MV,Jadhav SL
Journal of Drug Delivery and Therapeutics , 2012,
Abstract: Excellent impervious nature of skin is the greatest challenge that has to be overcome for successfully delivering drug molecules to the systemic circulation by this route. Various formulation approaches used to systemically deliver drug molecules include use of prodrugs/lipophilic analogs, permeation enhancers, sub saturated systems and entrapment into vesicular systems. Further, the adhesive mixture, physical system of the delivery system and release liner influence drug release and its permeation across the skin. The novel microneedle dual-delivery method combines the advantages of hypodermic syringes and transdermal patches. Composed of dozens to hundreds of hollow microneedles, a (1–2) cm2 transdermal patch is applied to the skin to increase its permeability. Arrays of microneedles that are 100–1000 μm in length poke through the top layers of skin and allow micron-scale drugs to pass into the body. The needles are too small to stimulate nerve endings; patients wouldn’t feel any pain when a microneedle injection is performed. This review gives an overview of microneedles for drug delivery applications. The concept of miniaturized needles is presented and defined. Specific requirements for microneedles aimed for transdermal drug delivery are discussed and the scope is delimited. Some of the basic microfabrication methods used to fabricate microneedles is introduced and microneedles for drug delivery presented so far are reviewed and commented.
MICRONEEDLES IN TRANSDERMAL DRUG DELIVERY: AN UNIQUE PAINLESS OPTION
Chanda Silpi,Bagga Manish,Tiwari Raj Kumar
International Research Journal of Pharmacy , 2011,
Abstract: The outermost layer of skin, the stratum corneum, has developed unnerving physical and immunological barrier properties that prevent infiltration of noxious chemicals and pathogens. Consequently, transdermal delivery of medicaments is currently restricted to a limited number of low molecular weight drugs to enter the skin at successful therapeutic rates. As a result, there has been significant recent interest in providing strategies that disrupt or dodge the principal physical barrier, the stratum corneum, for the efficient cutaneous delivery of macromolecular and nucleic acid based therapeutics. Recently, the use of micron-scale needles in increasing skin permeability has been proposed and shown to dramatically increase transdermal delivery, especially for macromolecules. Using the tools of the microelectronics industry, micro-needles have been fabricated with a wide range of sizes, shapes and materials. These strategies include: Micro-needles, Macroflux . A micro-needle-based drug delivery system is pain free administration, easy to use, discrete, continuous and controlled release system. This review compile the current advancement and literature regarding the fabricated micro-needles used for enhancing Transdermal Drug Delivery System and other structure based techniques.
Ionic Liquids as Potential and Synergistic Permeation Enhancers for Transdermal Drug Delivery
Lisa C. du Toit,Pierre P. D. Kondiah,Pradeep Kumar,Thashree Marimuthu,Viness Pillay,Yahya E. Choonara,Zainul Sidat
- , 2019, DOI: 10.3390/pharmaceutics11020096
Abstract: Transdermal drug delivery systems (TDDS) show clear advantages over conventional routes of drug administration. Nonetheless, there are limitations to current TDDS which warrant further research to improve current TDD platforms. Spurred by the synthesis of novel biodegradable ionic liquids (ILs) and favorable cytotoxicity studies, ILs were shown to be a possible solution to overcome these challenges. Their favorable application in overcoming challenges ranging from synthesis, manufacture, and even therapeutic benefits were documented. In this review, said ILs are highlighted and their role in TDDS is reviewed in terms of (a) ILs as permeation enhancers (single agents or combined), (b) ILs in drug modification, and (c) ILs as active pharmaceutical ingredients. Furthermore, future combination of ILs with other chemical permeation enhancers (CPEs) is proposed and discussed
Transdermal Drug Delivery System- Design and Evaluation
Eseldin Keleb,Rakesh Kumar Sharma,Esmaeil B Mosa,Abd-alkadar Z Aljahwi
International Journal of Advances in Pharmaceutical Sciences , 2011, DOI: 10.5138/171
Abstract: The human skin is a readily accessible surface for drug delivery. Skin of an average adult body covers a surface of approximately 2 m 2 and receives about one-third of the blood circulating through the body. Over the past three decades, developing controlled drug delivery has become increasingly important in the pharmaceutical industry. The human skin surface is known to contain, on an average, 10-70 hair follicles and 200-250 sweat ducts on every square centimeters of the skin area. It is one of the most readily accessible organs of the human body. The potential of using the intact skin as the port of drug administration to the human body has been recognized for several decades, but skin is a very difficult barrier to the ingress of materials allowing only small quantities of a drug to penetrate over a period of time. During the past decade, the number of drugs formulated in the patches has hardly increased, and there has been little change in the composition of the patch systems. Modifications have been mostly limited to refinements of the materials used. The present article reviews the selection of drug candidates suitable to be formulated as Transdermal system and the methods of evaluation. Keywords:- Transdermal; Drug Delivery; TDDS
Polymeric Biomaterial Based Hydrogels for Biomedical Applications  [PDF]
Nabanita Saha, Aamarjargal Saarai, Niladri Roy, Takeshi Kitano, Petr Saha
Journal of Biomaterials and Nanobiotechnology (JBNB) , 2011, DOI: 10.4236/jbnb.2011.21011
Abstract: This paper focuses on the significant properties of hydrogels prepared with polymeric biomaterials: solely biopolymers (gelatin (G) and sodium alginate (SA) as base polymer) or in combination with synthetic and bio polymers (polyvinylpyrrolidone (PVP) and carboxymethylcellulose (CMC)) for biomedical application. Four kinds of hydrogels: G/SA, G/SA/SB (without and with seabuckthron oil (SB)) and PVP/CMC, PVP/CMC/BA (without and with boric acid (BA)) which are different from each other concerning shape, size, color, texture and properties point of view were achieved. G/SA and G/SA/SB hydrogels vary from pale yellow to orange and a little rubber like having 42-48 % moisture. On the other hand, PVP/CMC and PVP/CMC/BA hydrogels are transparent and soft gel like containing about 90-95% moisture. Both G/SA and PVP/CMC hydrogels show similar trend of viscoelastic behaviour within whole range of measured angular frequency (0.1 – 100 rad.s-1). However, the presence of BA in PVP/CMC/BA, increases the storage modulus, loss modulus and complex viscosity of hydrogel, and the presence of SB in G/SA/SB demonstrates the decrease all of these values. G/SA based hydrogel possesses natural antimicrobial property whereas PVP/CMC based hydrogel needs to incorporate antimicrobial agent to comprise antimicrobial property within the hydrogel. G/SA hydrogels show water absorption capacity until 90 min whereas PVP/CMC hydrogels are able to absorb water steadily till 240 min. Finally, it can be mentioned that all four hydrogels: G/SA, G/SA/SB, PVP/CMC, PVP/CMC/BA which meet the basic requirements of hydrogel dressings, could be recommended as dressing materials for healing of burn or cut wound as well as a tool for transdermal drug delivery.
Liposomes Carrying Diclofenac Diethylammonium: A Penetrability and Permeation Study  [PDF]
Adriana Camino, Anyoli Taly, Cirana Rodriguez, Alfredo Inatti, Evelyn Pena, Xenon Serrano
Journal of Biosciences and Medicines (JBM) , 2024, DOI: 10.4236/jbm.2024.1212016
Abstract: This study investigated whether liposomes could enhance the permeation and penetration of diclofenac diethylammonium. For this, a 1.16% diclofenac diethylammonium liposome gel formulation was developed (Grupo Leti, S.A.V.). In vitro and ex vivo tests were conducted to analyze the diffusion and penetration profiles of the formulation. The profiles obtained were compared with a commercially available product, DiAnalper gel (Pharmetique Labs). The in vitro test was assessed in a Franz diffusion cell system using a dialysis membrane. The cumulative amount of drug permeated after 24 h demonstrated a significantly (p < 0.05) enhanced diffusion for the liposomal gel formulation compared to the commercial product. Specifically, the liposomal gel exhibited values of 710.56 ± 12.23 μg/cm2, whereas the commercial formulation yielded values of 371.00 ± 3.54 μg/cm2. These findings were further supported by consistent results in the percentage of drug release, flux, and permeability coefficient, all indicating a notable improvement in diffusion associated with the liposomal gel formulation. The tape stripping assay performed on pig ear skin demonstrates a statistically significant difference (p < 0.05) between the penetration transport of the diclofenac from liposome gel formulation (1413.95 ± 250.51 μg) and the conventional product (202.36 ± 18.07 μg) the liposomal formulation was able to cross de stratum corneum and deliver a high amount of drug to the skin. These findings demonstrated that incorporating diclofenac into a liposomal system significantly improved the drug delivery, which could confer an advantage for clinical uses.
OPTIMIZATION TECHNIQUES IN TRANSDERMAL DRUG DELIVERY SYSTEM
Shikha Deshwal et al
International Journal of Pharmaceutical Sciences and Research , 2012,
Abstract: Transdermal drug technology specialists are continuing to search for new methods that can effectively and painlessly deliver larger molecules in therapeutic quantities to overcome the difficulties associated with the oral route. Transdermal Drug Delivery System (TDDS) is the system in which the delivery of the active ingredients of the drug occurs by the means of skin. Skin is an effective medium from which absorption of the drug takes place and enters in to circulatory system. Various types of transdermal patches are used to incorporate the active ingredients into the circulatory system via skin. The patches have been proved effective because of its large advantages over other controlled drug delivery systems. This review article covers a brief outline of various components of transdermal patch, applications of transdermal patch, their advantages, disadvantages, when the transdermal patch are used and when their use should be avoided, types of transdermal patch, recent techniques for enhancing TDDS
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