Vitamin K1-loaded lipid-core nanocapsules: physicochemical characterization and in vitro skin permeation.
BACKGROUND
The incorporation of substances in nanocarriers can modulate and/or manage their delivery profiles (immediate or sustained) and permeation through skin. Consequently, drug nanencapsulation intended for topical treatment can reduce the systemic absorption of the substance.


OBJECTIVE
To obtain and characterize vitamin K1-loaded lipid core nanocapsules as well as to determine whether the nanoencapsulation influences the skin permeation of this vitamin.


METHODS
The skin permeation study was performed by means of Franz-type diffusion cells followed by the tape stripping and retention techniques. The vitamin K1-loaded lipid core nanocapsules were obtained by the preformed polymer precipitation method and the particles were characterized.


RESULTS
The nanocapsules presented average diameter of 211 ± 2 nm, pH of 5.7 ± 0.3, zeta potential of -14.9 ± 0.6 mV and drug content of 10.2 mg/mL (102.1%). The physical stability of the nanocapsule suspension was verified using multiple light backscattering analysis. The amount of vitamin K1 in the dermis after 8 h of drug permeation was higher when the nanocapsules were applied compared to the control. Moreover, retention in the outermost skin layer and a decrease in the skin permeation to the receptor compartment due to the nanoencapsulation were observed.


CONCLUSIONS
Thus, nanoencapsulation can lead to the selective permeation of vitamin K1 through the skin.
Postgraduate Program in Pharmaceutical Sciences, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Ana Luiza M
AL
da Silva
Renata V
RV
Contri
Denise S
DS
Jornada
Adriana R
AR
Pohlmann
Silvia S
SS
Guterres
D000818:Animals; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics*; D005260:Female; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry; D053769:Nanocapsules / Q000737:chemistry*; D010316:Particle Size; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013552:Swine; D014783:Viscosity; D010837:Vitamin K 1 / Q000493:pharmacokinetics*; D014815:Vitamins / Q000493:pharmacokinetics*
D004337:Drug Carriers; D008055:Lipids; D053769:Nanocapsules; D011108:Polymers; D014815:Vitamins; D010837:Vitamin K 1