Formulation...Sudhir Bharadwaj et al.through the body. An average human skin surface is known to contain, on the average 40-70 hair folliclesand 200-300 sweat ducts on every square centimeter <strong>of</strong> the skin 1 . Although skin has been dividedhistologically into the stratum corneum, the living epidermis and the dermis, collectively it can beconsidered a laminate <strong>of</strong> barrier, permeation <strong>of</strong> this laminate can occur by diffusion via:a. Transcellular penetration (across the cells)b. Intracellular penetration (between the cells)c. Transappendageal penetration (via hair follicles, sweat and sebum glands) 2, 3A myriad <strong>of</strong> medicated product are applied to the skin or readily accessible mucous membrane that insome way either augment or restore a fundamental function <strong>of</strong> a skin or pharmacologically modulate anaction in the underlined tissues. Such products are referred as topical or dermatological product 4 .1.RATIONAL APPROACH TO TOPICAL FORMULATIONS 5<strong>Topical</strong> <strong>for</strong>mulation can be used to:• Manipulate the barrier function <strong>of</strong> the skin, e.g., topical antibiotics and antibacterial help a damagedbarrier to ward <strong>of</strong>f infection, sun screening agents and the horny layer protect the viable tissues fromU.V. radiation.• Direct <strong>drug</strong>s to the viable skin tissues without using oral, systemic or other routes <strong>of</strong> therapy, e.g.,anaesthetic, anti-inflammatory, antipruritic and antihistaminics <strong>drug</strong>s are to be delivered to viableepidermis and dermis.• For skin appendage treatment, e.g., antiperspirants, exfolients and depilatories are to be delivered tothe skin appendages.• Deliver <strong>drug</strong>s <strong>for</strong> systemic treatment, e.g., transdermal therapeutic systems provide systemic therapy<strong>for</strong> motion sickness, angina and hypertension.1.1. TOPICAL GELSThe term ‘<strong>Gel</strong>’ was introduced in the late 1800 to name some semisolid material according to theirphysiological characteristics rather than molecular composition.<strong>Gel</strong>s are semisolid systems in which a liquid phase is constrained within a three dimensional polymericmatrix <strong>of</strong> natural or synthetic gums in which a high degree <strong>of</strong> physical or chemical cross linking has beenestablished 6 .The U.S.P. defines gels 7 as a semisolid system consisting <strong>of</strong> dispersion made up <strong>of</strong> either small inorganicparticle or large organic molecule enclosing and interpenetrated by liquid. The inorganic particles <strong>for</strong>m athree-dimensional ‘house <strong>of</strong> cards’ structure. <strong>Gel</strong>s consist <strong>of</strong> two-phase system in which inorganicparticles are not dissolved but merely dispersed throughout the continuous phase and large organicparticles are dissolved in the continuous phase, randomly coiled in the flexible chains. These chains areentangled with each other and shown as a single phase. The interaction between the colloidal phase,(inorganic or organic) set up the ‘structural viscosity’.Most topical gels are prepared with organic polymers, such as carbomers, that impart an aestheticallypleasing, clear, sparkling appearance to the products and are easily washed <strong>of</strong>f from the skin with water.The type <strong>of</strong> base used in <strong>for</strong>mulating a topical dermatological product greatly influences its effectiveness.Bases containing large amounts <strong>of</strong> oleaginous substances provide an emollient effect to dry irritated skin.More importantly, bases made up <strong>of</strong> non-volatile oleaginous substances (e.g. hydrocarbon bases) can <strong>for</strong>m857 J. Chem. Bio. Phy. Sci. Sec.B, 2012, Vol.2, No.2,856-867
Formulation...Sudhir Bharadwaj et al.an occlusive barrier on the skin that prevents escape <strong>of</strong> moisture from the skin into the environment. As aresult, moisture accumulates between the skin and the ointment layer that cause hydration <strong>of</strong> the stratumcorneum. Hydration <strong>of</strong> stratum corneum all ‘opening up’ <strong>of</strong> intra and inter-cellular channels and pathway<strong>for</strong> easier passage <strong>of</strong> <strong>drug</strong> molecules. Additionally, the moisture layer provides a medium <strong>for</strong> dissolution<strong>of</strong> the <strong>drug</strong> that is otherwise dispersed as fine particles in the ointment base. Since only the dissolved <strong>drug</strong>presented to the skin, as an individual molecular entity is able to enter the stratum corneum, skinocclusion generally results in enhanced percutaneous <strong>drug</strong> absorption 8 .1.1.1. Classification<strong>Gel</strong>s are classified mainly by two methods based on 9 :a. Nature <strong>of</strong> colloid phasei. Inorganic gelsii.Organic gelsb. Based on nature <strong>of</strong> solventi. Aqueous gelsii.Non aqueous gels1.1.2. <strong>Gel</strong> <strong>for</strong>ming substances 10Polymers are used to give the structural network, which is essential <strong>for</strong> the preparation <strong>of</strong> gels. <strong>Gel</strong><strong>for</strong>ming polymers are classified as follows:1. Natural polymera. Proteinsi. Collagenii. <strong>Gel</strong>atinb. Polysaccharidesi. Agarii. Alginic acidiii. Sodium or Potassium carrageenaniv. Tragacanthv. Pectinvi. Guar Gumvii. Cassia toraviii. Xanthinix. <strong>Gel</strong>lum Gum2. Semisynthetic polymersa. Cellulose derivativesi. Carboxymethyl cellulose858 J. Chem. Bio. Phy. Sci. Sec.B, 2012, Vol.2, No.2,856-867