title: Terpene composited lipid nanoparticles for enhanced dermal delivery of all-trans-retinoic acids.
abstract: In the present study, terpene composited lipid nanoparticles and lipid nanoparticles were developed and evaluated for dermal delivery of all-trans-retinoic acids (ATRA). Terpene composited lipid nanoparticles and lipid nanoparticles were investigated for size, size distribution, zeta potential, entrapment efficiency, photostability, and cytotoxicity. In vitro skin permeation of ATRA lipid formulations were also evaluated. To explore the ability of lipid nanocarriers to target the skin, the distribution of rhodamine B base in the skin was investigated using confocal laser scanning microscopy (CLSM). The results indicated that the physicochemical characteristics of terpene composited lipid nanoparticles influenced skin permeability. All lipid nanocarriers significantly protected ATRA from photodegradation and were non-toxic to normal human foreskin ﬁbroblast cells in vitro. Solid lipid nanoparticles containing 10% limonene (10% L-SLN) had the highest ATRA skin permeability. Terpene composited SLN and nanostructured lipid carriers (NLC) showed higher epidermal permeation of rhodamine B across the skin based on CLSM image analysis. Our study suggests that terpene composited SLN and NLC can be potentially used as dermal drug delivery carriers for ATRA.
authors.affiliation: Faculty of Pharmacy, Silpakorn University.
authors.forename: Ponwanit
authors.initials: P
authors.lastname: Charoenputtakun
authors.forename: Boonnada
authors.initials: B
authors.lastname: Pamornpathomkul
authors.forename: Praneet
authors.initials: P
authors.lastname: Opanasopit
authors.forename: Theerasak
authors.initials: T
authors.lastname: Rojanarata
authors.forename: Tanasait
authors.initials: T
authors.lastname: Ngawhirunpat
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry* / Q000633:toxicity; D004355:Drug Stability; D017815:Elapidae; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry* / Q000633:toxicity; D018613:Microscopy, Confocal; D053758:Nanoparticles / Q000737:chemistry* / Q000633:toxicity; D010316:Particle Size; D010539:Permeability; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption; D013499:Surface Properties; D034421:Sus scrofa; D013729:Terpenes / Q000737:chemistry* / Q000633:toxicity; D014018:Tissue Distribution; D014212:Tretinoin / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D004337:Drug Carriers; D008055:Lipids; D013729:Terpenes; D014212:Tretinoin