ISSN 2395-3411 Available online at www.ijpacr.com 102 ______________________________________________________________Review Article Topical Sprays: Novel Drug Delivery System Prakarsha Chavan, Amrita Bajaj and Akkshata Parab* Department of Pharmaceutics, SVKM’s Dr. Bhanuben Nanavati College of Pharmacy, Vile Parle (West), Mumbai - 400 056, Maharashtra, India. _________________________________________________________________________ ABSTRACT Topical drug delivery systems have been found to have many advantages over oral drug delivery systems such as avoidance of first pass metabolism, gastro intestinal irritability, slow onset of action, etc. The clinical evidence indicates that conventional topical formulations possess certain short comings like irritancy, allergies due to the variety of excipients used. This review deals with all detailed information regarding rational approach to novel topical formulations like topical/ transdermal sprays and their formulation, fabrication and evaluation parameters. Keywords: Topical sprays, Metered dose transdermal spray, Advanced Preservative Free Container. INTRODUCTION followed by fabrication of a drug delivery system Over the last few decades the treatment of that meets all the stringent needs that are illness has been accomplished by administering specific to the drug molecule (physicochemical drugs to human body via various other routes in and stability factors), the patient (comfort and addition to traditional oral and sublingual routes cosmetic appeal), the manufacturer (scale up like rectal, parenteral, topical, inhalation, etc. and manufacturability) and most important the With the advent of new era of pharmaceutical economy. Topical preparations are used for the dosage forms, topical drug delivery systems localized effects at the site of their application by have established themselves as integral part of virtue of drug penetration into the underlying novel drug delivery products. Topical drug layers of skin or mucous membranes3. delivery systems (TDDS) are gaining increase in popularity and several drugs have been Advantages of Topical Drug Delivery successfully delivered by topical/transdermal Systems4 route for both local and systemic action. Avoidance of first pass metabolism. Topical/transdermal drug delivery systems offer Convenient and easy to apply. the non-invasive delivery of medication from the Achievement of efficacy with lower total daily surface of skin, the largest and most accessible dosage of drug due to continuous drug organ of human body-through its layers, to the input. circulatory system1. Topical delivery is the Avoidance of gastro-intestinal application of a drug containing formulation to incompatibility. the skin to directly treat cutaneous disorders or Improve patient compliance. other effects within the skin. Topical drug delivery systems offer many advantages over Limitations of Topical Drug Delivery conventional injection and oral methods. It Systems5 reduces the load that the oral route commonly Skin irritation and contact dermatitis may places on the digestive tract and liver. It occur due to the drug and/or excipients. enhances patient compliance and minimizes Can be used only for drugs which require harmful side effects of a drug caused due to very small plasma concentration for action. temporary overdose2. Drugs of larger molecular size are not easy The development of TDDS is multidisciplinary to be absorbed by the skin. activity that encompasses fundamental feasibility studies starting from the selection of Topical dosage forms, an alternative to drug molecule to the demonstration of sufficient conventional formulations, are becoming popular drug flux in an ex vivo and in vivo model because of their unique advantages. The topical International Journal of Pharma And Chemical Research I Volume 2 I Issue 2 I Apr – Jun I 2016 ISSN 2395-3411 Available online at www.ijpacr.com 103 drug delivery systems are mainly used in pain Introduction to Topical sprays management, contraception, infections, The history of aerosol technology is traced back allergies, inflammation and urinary incontinence. to the early years of the twentieth century. The Various novel topical dosage forms include: principles of aerosol technology were applied to Topical gels the pharmaceutical aerosols in early 1950s. The Topical sprays topical aerosol products were intended for Topical patches application for treatment of burns, minor cuts, Topical films bruises, infection and various dermatological conditions. Historically, developments in topical Topical gels drug delivery have been incremental, focusing Gels are transparent to opaque semisolids on overcoming problems associated with the containing a high ratio of solvent to gelling barrier properties of the skin, reducing skin agent. Gels are created by entrapment of large irritation rates and improving the aesthetics amounts of aqueous or hydroalcoholic liquid in a associated with conventional topical drug network of colloidal solid particles, consisting of delivery systems. Regardless of the inorganic substances, such as aluminum salts or transdermal/topical drug delivery systems in organic polymers of natural or synthetic origin. development, the patient acceptability from an Depending upon the nature of colloidal aesthetic, safety and non-irritancy perspective substance and the liquid in the formulation, the will remain the main focus for the newer gels range in appearance from entirely clear to products entering the market. The non-invasive opaque. Most topical gels are prepared with character of transdermal drug delivery makes it organic polymers, such as carbomers, that accessible to a wide range of patient population impart an aesthetically pleasing, clear, and is a highly acceptable option for drug sparkling appearance to the product, and are dosing. easily washed off the skin with water6. Problems with existing technology Topical patches Transdermal/topical drug delivery systems (TDDS) such as patches, creams and gels still A topical patch is a medicated adhesive patch 8 that is placed on the skin to deliver a specific suffer from some limitations . The precision of dose of medication through the skin and into the dosing is particularly an issue with creams and bloodstream. The first commercially available gels, especially as it has also been topical prescription patch was approved by the demonstrated that altering the dose applied per U.S. Food and Drug Administration in December surface area can affect the drug delivery profile, although conflicting effects have been observed 1979, namely scopolamine patch for motion 9 sickness7. The adhesive is covered by a release when the area of application is increased . liner, which needs to be peeled off before Although precision of dosing might be less of an applying the patch on the skin. issue in patch systems, there is relatively little flexibility available for the dosing. Variability of Topical films dosing has also been highlighted as an issue with TDD systems. Most studies have focused These are medicated transparent polymeric 10 films similar to topical patches. The only on the intra-site variability of dosing that many difference is that films do not contain adhesive have attributed to the different levels of skin polymer. hydration found at various anatomical sites. It has also been shown that variations in Topical sprays temperature, possibly due to local Topical sprays are dosage forms in which microcirculation changes in the skin, can affect polymeric solution of drug is sprayed over the the drug delivery profile from TDDS. Variability intact skin so as to get a sustained release of of dosing has also been observed between different skin types, skin of different aged drug from the polymeric matrix. The drug is 11 12 present in saturated form in the polymer matrix. patients and diseased skin . As the organic solvent vehicle evaporates, Psychological stress has also been shown to slowly the drug diffuses through the polymer impact skin barrier recovery. The relatively high matrix and passes from the skin barrier. skin irritation rates that were associated with the earlier transdermal patches have been somewhat reduced, but the inherent occlusive nature of the products still dictates that this International Journal of Pharma And Chemical Research I Volume 2 I Issue 2 I Apr – Jun I 2016 ISSN 2395-3411 Available online at www.ijpacr.com 104 remains an issue for TDDS13. The occurrence of component also enables the formulation to have sensitization reported has been up to 50% with uniform distribution on the skin over a defined clonidine patch and seen to increase with time of area after application, without leaving excess exposure14. As consumers become increasingly vehicle. Hence, this ensures that the dose can educated about product options, their be administered in a precise and highly expectations regarding skin irritation rates and reproducible manner and that aesthetic value patch size have also been increased. From the and transference issues are avoided. The patient‟s perspective, the large surface area for evaporation of some of the vehicle leads to an application, particularly for gels and creams, increase in concentration of the active drug and which is required to produce adequate dosing hence enhanced partitioning into the stratum levels, can also translate into aesthetic corneum. concerns. It is crucial that formulators consider The non-volatile component prevents the drug the aesthetics of the product after application, to from precipitating
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