Lyotropic liquid crystal mesophases as transdermal delivery systems for lipophilic drugs: A comparative study

• Published in: International journal of pharmaceutics Vol. 636; p. 122853
• Main Authors: de Araujo, Guilherme Rodolfo Souza, Azevedo Lima, Odeanny Vitória, Barreto Neujahr, João Pedro, Matos, Saulo Santos, de Souza, Thalisson Amorim, dos Santos, Aline Martins, Chorilli, Marlus, de Souza Araujo, Adriano Antunes, Duarte, Marcelo Cavalcante, da Cunha Gonsalves, Joyce Kelly Marinheiro, de Souza Nunes, Rogéria, dos Santos, Marcio Roberto Viana, Vitorino Sarmento, Victor Hugo, Moreira Lira, Ana Amélia
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 05-04-2023
• Subjects: Administration, Cutaneous; Liquid Crystals - chemistry; Lyotropic liquid crystal; Nanostructured system; Pharmaceutical nanotechnology; Pharmaceutical Preparations; Scattering, Small Angle; Skin; Transdermal drug delivery system; X-Ray Diffraction; Nanostructured system; Pharmaceutical nanotechnology; Transdermal drug delivery system; Lyotropic liquid crystal
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2023.122853

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The present work aimed to evaluate different Liquid Crystal Mesophases (LCM) as transdermal drug delivery systems (TDDS) for nifedipine (NFD), a lipophilic drug model. The formulations composed of water, Citrus sinensis essential oil (CSEO), PPG-5-CETETH-20, and Olive oil ester PEG-7 were obtained and characterized by polarized light microscopy (PLM), rheology, small-angle x-ray scattering (SAXS), Fourier transform infrared coupled with an attenuated total reflection accessory (FTIR-ATR) and in vitro assays: bioadhesion, drug release, skin permeation, and retention tests. As a result, changes in component proportions led to several transparent viscous systems with an anisotropic profile. PLM and SAXS proved the presence of lamellar (S1), hexagonal (S3), and lamellar + hexagonal (S2) LCM, and rheology showed a high viscoelasticity profile. LCMs were able to adhere to the skin, and S2 achieved higher adhesion strength. NFD (5 mg/mL) has not modified the organization of LCMs. Results also showed that S3 promoted higher permeation and retention and higher disorganization of stratum corneum lipids, which is the main permeation-enhancing mechanism. Thus, the formulations obtained can carry and improve drug delivery through the skin and are promising TDDS for lipophilic drug administration, such as NFD.