Seyed Alireza Mor tazavi, Ph.D. Professor of Pharmaceutics School of Pharmacy Shaheed Beheshti University of Medical Sciences • Cosmetic products: • “Articles intended to be rubbed, poured, sprinkled, or sprayed on, introduced into, or otherwise applied to the human body or any part there of for cleansing, beautifying and promoting attractiveness, or altering the appearance.” • Cosmeceuticals: Antidandruff shampoos, toothpastes containing fluoride, anti-acne products, sunscreens, deodorants with an antiperspirant effect, moisturizers with sunscreen effect, make ups with sun-protection claims Popular Semi-solid dosage forms for topical application • Creams • Ointments • Gels • Pastes Bases and Vehicles Lanolin, Eucerin, Glyceryl monostearate, Cetyl alcohol, Stearyl alcohol, Spermaceti, Liquid Paraffin (mineral oil), Hard Paraffin, White soft Paraffin (Vaseline, Petrolatum), White and Yellow wax, PEG, Glycerin, etc.
Simple Ointment (Ointment USP)
Wax (white or yellow) 50g Petrolatum (white or yellow) 950g
PEG Ointment (USP)
PEG 400 600g PEG 3350 400g Hydrophilic Petrolatum Cholesterol 3g Stearyl alcohol 3g White wax 8g White petrolatum to 100g
(Protective and water absorbent base)
Hydrophilic ointment (washable o/w emulsion) White petrolatum 25 g Stearyl alcohol 25 g Sodium lauryl sulphate 1g Propylene glycol 12 g Methyl paraben 0.025 g Propyl paraben 0.015 g Purified water to 100 g Important considerations • Selection of vehicle and additives (skin type and place, age, duration of use) • Interactions and incompatibilities • Substantivity, texture and viscosity • Preservation (Preservative and Antioxidant) • Stability • Efficacy • Irritation testing Special issues regarding creams • Cleansing creams and lotions (avoid excessive use, can remove skin lipids leaving skin dry) • The use of non-ionic emulsifiers in formulations (tweens and spans, stearates, cetyl alcohol) • Cold cream (w/o, cooling effect) • Light creams (water washable, o/w) • Night creams (spread easily, soft, remain in place, high oil content, w/o emulsion, reduce TEWL and a hydrating and emollient effect, addition of anti-aging compounds) • Moisturizer creams [keep skin soft and smooth, contain humectants for hydrating creams, o/w, occlusive creams, emollient creams and ointments (w/o)] • Vitamin-containing creams Vit. A (e.g. Retinol, Retinyl esters and Retinaldehyde, sebum formation, Photodamage, anti-wrinkle and anti-aging, used in amounts less than 1%) Vit. B3 (e.g. nicotinic acid, nicotinamide, nicotinate esters, help to reduce TEWL, nicotinamide helps to produce collagen) Vit. B5 (Pantothenic acid and Panthenol, healing effect, skin hydration, Emollient, increased dermal elasticity, anti-inflammatory and anti-itching effect) Vit. C and Vit. E (antioxidant effect, anti-aging) Vit. D (skin keratinization and skin repair) Vit. K (reduce darkness around eyes) • Vanishing creams (disappear rapidly from skin, form a clear layer on skin, stearic acid, cetyl alcohol, o/w) • Skin lighteners Cream formulation, remove skin stains, freckle, Hydroquinone 1.5 – 2 % popular and 5% or even higher Aloesin, Arbutin, Ellagic acid, Kojic acid 1%, Azelaic acid 15 – 20% Vit. C and E, Silymarin, Alpha lipoic acid Popular liquid dosage forms for topical application
• Various Solutions • Lotions (suspension or emulsion) • Collodions Selection of solvent/co-solvent 1- Complete miscibility 2- Clarity 3- Viscosity 4- Toxicity 5- Compatibility with other components