title: Nanostructured lipid carriers for the topical delivery of tretinoin.
abstract: Cosmetic skin care products currently in the market demonstrate an increasing trend toward antiaging products. Selection of the right formulation approach is the key to successful consumer acceptance. Nanostructured lipid carriers (NLCs) for dermal application can render added benefits to the formulation. Tretinoin a derivative of vitamin A, is a retinoid with anti-aging and anti-acne potential. The present study was aimed at formulating NLCs of tretinoin for reducing the skin irritation potential, increasing the drug loading capacity and prolonging the duration of action. The NLCs were optimized using the response surface methodology based on the particle size. Preliminary study, suggested the use of stearic acid, oleic acid, Tween 80 and Span 60 as solid lipid, liquid lipid and surfactants respectively formed a stable dispersion. NLCs of tretinoin were prepared by hot melt microemulsion and hot melt probe sonication methods. The properties of the optimized NLCs such as morphology, size, Zeta potential, stability and in vitro drug release were investigated. Tretinoin loaded NLCs in carbopol gel showed a sustained release pattern with isopropyl alcohol as the receptor fluid compared to the marketed gel using Franz diffusion cells. Eight prepared gel formulations tested were found to follow the Higuchi model of drug release. Stability studies indicated that the formulations stored at refrigeration and room temperature showed no noticeable differences in the drug content and release profiles in vitro, after a period of 4 weeks. In vivo skin irritation test on male Wister rats indicated no irritation or erythema after application of the NLCs loaded gel repeated for a period of 7 days compared to the application of marketed tretinoin gel which showed irritation and slight erythema within 3 days. The results showed that the irritation potential of tretinoin was reduced, the drug loading was increased and the drug release was prolonged by the incorporation into the NLCs.
authors: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576104, Karnataka, India. Electronic address: vivekghatem@gmail.com.
authors: Vivek M
authors: VM
authors: Ghate
authors: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576104, Karnataka, India.
authors: Shaila A
authors: SA
authors: Lewis
authors: Department of Pharmaceutics, Shree Devi College of Pharmacy, Kenjar, Mangalore 570142, Karnataka, India.
authors: Prabhakara
authors: P
authors: Prabhu
authors: Department of Pharmaceutics, Shree Devi College of Pharmacy, Kenjar, Mangalore 570142, Karnataka, India.
authors: Akhilesh
authors: A
authors: Dubey
authors: Department of Pharmaceutics, Shree Devi College of Pharmacy, Kenjar, Mangalore 570142, Karnataka, India.
authors: Nilkumar
authors: N
authors: Patel
mesh_terms: D000152:Acne Vulgaris / Q000188:drug therapy; D000287:Administration, Topical; D000818:Animals; D002152:Calorimetry, Differential Scanning; D002784:Cholesterol / Q000737:chemistry; D003102:Colloids / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004655:Emulsions; D005782:Gels / Q000737:chemistry; D006601:Hexoses / Q000737:chemistry; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry; D019301:Oleic Acid / Q000737:chemistry; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012176:Retinoids / Q000008:administration & dosage; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013229:Stearic Acids / Q000737:chemistry; D013696:Temperature; D014212:Tretinoin / Q000737:chemistry*; D014801:Vitamin A / Q000737:chemistry
chemical_list: D003102:Colloids; D004337:Drug Carriers; D004655:Emulsions; D005782:Gels; D006601:Hexoses; D008055:Lipids; D011136:Polysorbates; D012176:Retinoids; D013229:Stearic Acids; D014801:Vitamin A; D019301:Oleic Acid; C031183:stearic acid; D014212:Tretinoin; D002784:Cholesterol; C009298:sorbitan monostearate
keywords: Cholesterol (PubChem CID: 5997); NLCs; Nanostructured lipid carriers; Oleic acid (PubChem CID: 445639); Optimization; Skin irritation; Span 60 (PubChem CID: 14928); Stearic acid (PubChem CID: 5281); Tretinoin; Tretinoin (PubChem CID: 444795); Tween 20 (PubChem CID: 86289077); Tween 80 (PubChem CID: 5281955)