Phytantriol-based lyotropic liquid crystal as a transdermal delivery system

Wan, Jun; Wang, Sheng-mei; Gui, Zhiping; Yang, Zhuanzhuan; Shan, Qianqian; Chu, Xiaoqin; Gui, Shuangying; Yang, Ye

doi:10.1016/j.ejps.2018.09.018

Cited by 31 publications

(13 citation statements)

References 30 publications

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“…This may be due to the good biocompatibility between biofilm-like lipid carriers and corneal epithelial cells, resulting in more easily transport and an elevated solubility of encapsulated drug molecules through the corneal barriers. Besides, PYT, as an amphiphilic lipid, has its own osmotic promoting effect could penetrate across tight junctions to strengthen corneal epithelial permeability (Zhang et al., 2015; Chu et al., 2018; Wan et al., 2018). Surprisingly, the corneal permeability of H 2 gel is better than that of Q 2 gel, which is contrary to the results of in vitro release.…”

Section: Resultsmentioning

confidence: 99%

“…As such, these systems can be regarded as comfortable and promising drug delivery strategies (Yang et al., 2018). Recently, PYT-based LC gels were applied to the treatment of chronic diseases, such as periodontitis by injected into periodontal pocket (Cohen-Avrahami et al., 2010), rheumatoid arthritis for transdermal delivery (Wan et al., 2018) and liver cancer by injected into intra-arterial (Han et al., 2010), which have enhanced bioavailability and remarkably reduced systemic side effects.…”

Section: Introductionmentioning

confidence: 99%

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Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment

Wang

Zhang

et al. 2019

Drug Delivery

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The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q 2) and hexagonal (H 2) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, smallangle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3mtype Q 2 and H 2 phase, and both of them showed pseudoplastic fluid properties based on characterization techniques. In vitro release profiles suggested that PN could be sustainably released from LC gels within 48 h. Compared with eye drops, Q 2 and H 2 gel produces a 5.25-fold and 6.23-fold increase in the P app value (p < .05), respectively, leading to a significant enhancement of corneal penetration. Furthermore, a good biocompatibility and longer residence time on precorneal for LC gels confirmed by in vivo animal experiment. Pharmacokinetic studies showed that LC gels could maintain PN concentration in aqueous humor for at least 12 h after administration and remarkably improve the bioavailability of drug. Additionally, in vivo pharmacodynamics studies indicated that LC gels had a more significant intraocular pressure-lowering and miotic effect compared to eye drops. These research findings hinted that LC gels would be a promising pharmaceutical strategy for ocular application to enhance the efficacy of anti-glaucoma.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment

Wang

Zhang

et al. 2019

Drug Delivery

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“…It was reported that the liquid crystal structure of the formulations affected the biomembrane permeability of the entrapped drugs. 25) The M 70 SSL preparation rapidly formed two types of liquid crystal structures (reverse hexagonal structure and cubic structures with lm3m space group, shown in Fig. 3), which probably relates to the high TA permeability.…”

Section: Discussionmentioning

confidence: 96%

“…On the other hand, Nicolazzo et al have reported no enhancement effect by ethanol on the TA permeation through the buccal membrane. 24) The enhancement effect by ethanol would be strengthened or weakened by different formulations. Ethanol was added in the spray formulation to facilitate spraying into the oral cavity by decreasing the viscosity.…”

Section: Discussionmentioning

confidence: 99%

Development of Spray Formulations Applied to the Oral Mucosa Using Non-lamellar Liquid Crystal-Forming Lipids

Sugibayashi

Yamamoto

Itakura

et al. 2020

CHEMICAL & PHARMACEUTICAL BULLETIN

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We examined the physicochemical and biochemical properties of mono-O-(5,9,13-trimethyl-4tetradecenyl)glycerol ester (MGE), including ease of handling, high bioadhesiveness, quick and stable in vivo self-organization (forming a non-lamellar lyotropic liquid crystal [NLLC]), and high biomembrane permeation enhancement. We prepared MGE oral mucosa-applied spray preparations containing triamcinolone acetonide (TA), which is widely used in the treatment of stomatitis, and we examined the usefulness of the MGE preparations compared with commercially available oral mucosal application preparations containing 2,3-dihydroxypropyl oleate (1-mono(cis-9-octadecenoyl)glycerol (GMO) (previously studied as an NLLCforming lipid) preparation. As a result, the MGE preparation applied to the oral mucosa can rapidly formed an NLLC with reverse hexagonal or cubic structures, or a mixture, on contact with water. In addition, by adding hydroxypropyl cellulose to the MGE preparation, similar retention properties on the oral mucous membrane were obtained to that using marketed drug preparations. Furthermore, the MGE spray formulation on the oral mucosa showed an equivalent or higher TA release as well as oral mucous membrane permeability compared with commercial formulations. Because MGE forms a stable NLLC and is easy to handle compared with GMO, MGE was considered to be a useful pharmaceutical additive for a spray preparation applied to the oral mucosa in combination.

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“…However, in the entire scanning process, the values before and after G''' did not change significantly. In the frequency range of 0.01-0.05Hz, the viscosity modulus was dominant (G' > G'), but in the frequency range of 0.05-10Hz, the elastic modulus was dominant (G' > G'), It could be concluded that the external frequency changes will affect the viscoelasticity of the liquid crystal gel, and we can infer that the liquid crystal gel had less irritation to the eyes at low frequencies [43] . It could be concluded that the external frequency changes would affect the viscoelasticity of the liquid crystal gel, and we could deduce that the liquid crystal gel had less irritation to the eyes at low frequencies.…”

Section: Rheological Characterzationmentioning

confidence: 92%

In Situ Liquid Crystal Gel as a New Ophthalmic Drug Delivery System for Pilocarpine Nitrate: Improving Preocular Retention and Ocular Bioavailability

Wu¹,

Cao²,

Cai³

et al. 2021

Preprint

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The purpose of this article is to develop an in-situ liquid crystal gel that can be used as a novel ocular delivery system for pilocarpine nitrate (PN). The phytantriol (PT) -based in situ liquid crystal gels were prepared by a vortex method using PT, PEG400, Triglyceride (TAG) and water (in the ratio of 61.15:30:3.85:5, w/w). Firstly, the internal structure of the PN-loaded liquid crystal gel was characterized by polarizing microscope (PLM), small-angle X-ray scattering (SAXS), differential scanning calorimetry (DSC) and rheology. In vitro drug release behavior and ex vivo corneal permeation were investigated. Finally, eye irritation test，preocular residence time evaluation,were studied in vivo and compared with eye drops.Based on various characterization techniques, it is proved that the internal structure of the gel is a hexagonal phase.In vitro release results identified that PN could be released continuously from HII gel over a period of 24 h. The in vitro obvious permeability coefficient of HII gel was 3.19-fold (P < 0.01) higher than that of the eye drops. Compared with eye drops,the HII gel had good bioadhesion and displayed longer residence time on the eyeballs surface using fluorescent labeling technology.In addition, through Corneal hydration level and eye irritation test ., it is conjectured that HII gel will not cause eye irritation. In short, the formulation has the advantages of high efficiency, slow release and non-toxicity, and will become a promising pharmaceutical strategy to improve the efficacy of glaucoma.

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Phytantriol-based lyotropic liquid crystal as a transdermal delivery system

Cited by 31 publications

References 30 publications

Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment

Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment

Development of Spray Formulations Applied to the Oral Mucosa Using Non-lamellar Liquid Crystal-Forming Lipids

In Situ Liquid Crystal Gel as a New Ophthalmic Drug Delivery System for Pilocarpine Nitrate: Improving Preocular Retention and Ocular Bioavailability

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