The design of naproxen solid lipid nanoparticles to target skin layers.
The aim of the current investigation was to produce naproxen solid lipid nanoparticles (Nap-SLNs) by the ultrasonication method to improve its skin permeation and also to investigate the influence of Hydrophilic-lipophilic balance (HLB) changes on nanoparticles properties. The properties of obtained SLNs loaded with naproxen were characterized by photon correlation spectroscopy (PCS), transmission electron microscopy (TEM) and differential scanning calorimetry (DSC). FT-IR was also used to investigate any interaction between naproxen and the excipients used at the molecular level during the preparation of the SLNs. The performance of the formulations was investigated in terms of skin permeation and also the retention of the drug by the skin. It was found that generally, with increasing the lipid concentration, the average particle size and polydispersity index (PDI) of SLNs increased from 94.257±4.852nm to 143.90±2.685nm and from 0.293±0.037 to 0.525±0.038 respectively. The results also showed that a reduction in the HLB resulted in an increase in the PDI, particle size, zeta potential and entrapment efficiency (EE%). DSC showed that the naproxen encapsulated in the SLNs was in its amorphous form. The peaks of prominent functional groups of naproxen were found in the FT-IR spectra of naproxen-SLN, which confirmed the entrapment of naproxen in the lipid matrix. FT-IR results also ruled out any chemical interaction between drug and the chemicals used in the preparation of SLNs. The amount of naproxen detected in the receptor chamber at all the sampling times for the reference formulation (naproxen solution containing all surfactants at pH 7.4) was higher than that of the Nap-SLN8 formulation. Nap-SLN8 showed an increase in the concentration of naproxen in the skin layer with less systemic absorption. This indicates that most of the drug in Nap-SLN8 remains in the skin which can reduce the side effect of systemic absorption of the drug and increases the concentration of the drug at the site of the action.
Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Jafar
J
Akbari
Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Majid
M
Saeedi
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Katayoun
K
Morteza-Semnani
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Seyyed Sohrab
SS
Rostamkalaei
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Masoumeh
M
Asadi
Pharmacy Department, School of Applied Sciences, University of Huddersfield, Queensgate, Huddersfield, UK.
Kofi
K
Asare-Addo
Pharmaceutics Research Laboratory, School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, UK; Drug Applied Research Center and Faculty of Pharmacy, Tabriz Medical Sciences University, Tabriz, Iran. Electronic address: a.nokhodchi@sussex.ac.uk.
Ali
A
Nokhodchi
D000818:Animals; D002152:Calorimetry, Differential Scanning; D005989:Glycerides / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D008055:Lipids / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D009288:Naproxen / Q000494:pharmacology*; D011208:Powders; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects*; D012869:Skin Absorption / Q000187:drug effects; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
D005989:Glycerides; D008055:Lipids; D011208:Powders; C048159:glyceryl monostearate; D009288:Naproxen
DSC; FT-IR; Naproxen; Skin permeation; Solid lipid nanoparticles; Ultrasonication