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. 2018 Nov;13(6):518-526.
doi: 10.1016/j.ajps.2017.10.004. Epub 2017 Dec 7.

Enhanced transdermal delivery of meloxicam by nanocrystals: Preparation, in vitro and in vivo evaluation

Qin Yu  1 , Xiying Wu  1 , Quangang Zhu  1 , Wei Wu  1   2 , Zhongjian Chen  1 , Ye Li  3 , Yi Lu  1   2
Affiliations

Enhanced transdermal delivery of meloxicam by nanocrystals: Preparation, in vitro and in vivo evaluation

Qin Yu et al. Asian J Pharm Sci. 2018 Nov.

Abstract

Meloxicam (MLX) is efficient in relieving pain and inflammatory symptoms, which, however, is limited by the poor solubility and gastrointestinal side effects. The objective of this study is to develop a nanocrystal formulation to enhance transdermal delivery of MLX. MLX nanocrystals were successfully prepared by the nanoprecipitation technique based on acid-base neutralization. With poloxamer 407 and Tween 80 (80/20, w/w) as mixed stabilizers, MLX nanocrystals with particle size of 175 nm were obtained. The crystalline structure of MLX nanocrystals was confirmed by both differential scanning calorimetry and X-ray powder diffractometry. However, the nanoprecipitation process reduced the crystallinity of MLX. Nanocrystals increased both in vitro and in vivo transdermal permeation of MLX compared with the solution and suspension counterparts. Due to the enhanced apparent solubility and dissolution as well as the facilitated hair follicular penetration, nanocrystals present a high and prolonged plasma MLX concentration. And 2.58- and 4.4-fold increase in AUC0→24h was achieved by nanocrystals comparing with solution and suspension, respectively. In conclusion, nanocrystal is advantageous for transdermal delivery of MLX.

Keywords: Acid-base neutralization; Meloxicam; Nanocrystals; Nanoprecipitation; Transdermal delivery.

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Figures

Unlabelled image
Graphical abstract
Fig. 1
Fig. 1
(A) Effects of the types of stabilizer on particle size of MLX nanocrystals. (B) Particle size variation during storage at 4 °C from nanocrystals prepared with different types of stabilizers. Effects of (C) weight ratios of poloxamer 407/Tween 80 and (D) concentration of the mixed stabilizers on particle size of MLX nanocrystals.
Fig. 2
Fig. 2
Effects of MLX concentration on the particle size of nanocrystals.
Fig. 3
Fig. 3
Effects of (A) speed and (B) time of high speed shearing on the particle size of MLX nanocrystals.
Fig. 4
Fig. 4
Intensity distribution of MLX nanocrystals before (red) and after (blue) lyophylization.
Fig. 5
Fig. 5
SEM photographs of (A) MLX raw material and (B) nanocrystals.
Fig. 6
Fig. 6
DSC thermograms of (A) MLX nanocrystals, (B) physical mixture, (C) poloxamer 407 and (D) MLX raw material.
Fig. 7
Fig. 7
PXRD patterns of (A) MLX raw material, (B) physical mixture, (C) nanocrystals, (D) NaCl, and (E) poloxamer 407. Inset: partial enlargement of PXRD patterns of nanocrystals.
Fig. 8
Fig. 8
In vitro skin permeation profiles of MLX from nanocrystals, solution and suspensions. *, P < 0.05.
Fig. 9
Fig. 9
Plasma concentration versus time profiles of MLX post dermal administration of MLX nanocrystals, solution and suspensions. *, P < 0.05.
Fig. 10
Fig. 10
Dermal retention per unit skin area (Qr) versus time profiles of MLX post dermal administration of MLX nanocrystals, solution and suspensions. *, P < 0.05.
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