Liquid Crystalline Systems for Transdermal Delivery of Celecoxib: In Vitro Drug Release and Skin Permeation Studies

Abstract

Abstract. Liquid crystalline systems of monoolein/water could be a promising approach for the delivery of celecoxib (CXB) to the skin because these systems can sustain drug release, improve drug penetration into the skin layers and minimize side effects. This study evaluated the potential of these systems for the delivery of CXB into the skin based on in vitro drug release and skin permeation studies. The amount of CXB that permeated into and/or was retained in the skin was assayed using an HPLC method. Polarizing light microscopy studies showed that liquid crystalline systems of monoolein/water were formed in the presence of CXB, without any changes in the mesophases. The liquid crystalline systems decreased drug release when compared to control solution. Drug release was independent of the initial water content of the systems and CXB was released from cubic phase systems, irrespective of the initial water content. The systems released the CXB following zero-order release kinetics. In vitro drug permeation studies showed that cubic phase systems allowed drug permeation and retention in the skin layers. Cubic phase systems of monoolein/water may be promising vehicles for the delivery of CXB in/through the skin because it improved CXB skin permeation compared with the control solution.

Trans-resveratrol-loaded nonionic lamellar liquid-crystalline systems: structural, rheological, mechanical, textural, and bioadhesive characterization and evaluation of in vivo anti-inflammatory activity

“…First, the structural similarity between this system and skin cells may be responsible for the increase in drug penetration into deep layers of the skin after topical application. 12 Second, the surfactant or oil molecules can diffuse on the skin surface and act as permeation enhancers of Res, because they disrupt the lipid structure of the stratum corneum. 94 This facilitates diffusion across the barrier, which normally limits the penetration of substances.…”

“…[6][7][8][9][10][11] In this aspect, liquid crystals have been developed for cutaneous delivery of drugs. [12][13][14][15][16][17][18][19] Liquid crystals are systems that can be formed using lipids and amphiphilic molecules, which spontaneously reorganize into three-dimensional structures, such as emulsions, microemulsions, or liquid-crystalline (LC) mesophases (lamellar, hexagonal, and…”

Evaluation of critical parameters for in vitro skin permeation and penetration studies using animal skin models

“…The use of a cryoprotectant agent such as 10% glycerol was previously suggested (Liangpeng et al, 2011;Bravo et al, 2000;Richters et al, 1996) in order to avoid ice crystal formation and maintain the skin barrier function. However, there is no consensus yet about the use of a skin cryoprotectant agent and the storage time of frozen skin used for in vitro permeation/penetration studies (Petrilli et al, 2016;Estracanholli et al, 2014;Liangpeng et al, 2011;Barbero and Frasch, 2009).…”

“…Meanwhile, the quantification of the penetrated drug in each strip or in the aggregate strips depends on sensitivity of the analytical method. Therefore, most studies quantify the penetrated drug into SC using the aggregate of all tape strips (Campos et al, 2016;Estracanholli et al, 2014;Praça et al, 2011;Rossetti et al, 2010;Herkenne et al, 2006).…”

Self-Assembled Cubic Liquid Crystalline Nanoparticles for Transdermal Delivery of Paeonol

“…Cubic crystal phase can improve osmotic rate and sustained drug release in skin, and its good in situ biological adhesion characteristic comes from the similarity between the vulnerable temporary surface protection of an ulcer and the vulnerable layer of the liquid cubic crystal, which make it superior to other percutaneous drug delivery systems [ 19 ]. Estracanholli et al [ 20 ] and Peng et al [ 12 ] proved that the cubic crystal had good percutaneous penetration performance by dermal testing. Cubic crystal gel and nanoparticles both could be used in a transdermal delivery system, but the high adhesion and poor spreadability of the gel has limited its application [ 21 ].…”