Mucoadhesive System Formed by Liquid Crystals for Buccal Administration of Poly(Hexamethylene Biguanide) Hydrochloride

Souza, Carla; Watanabe, Evandro; Borgheti-Cardoso, Lívia Neves; Fantini, M.C.A.; Lara, Marilisa Guimarães

doi:10.1002/jps.24198

Cited by 45 publications

(31 citation statements)

References 60 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…20 MO are polar, amphiphilic lipids which have remarkable chemical and physical stability, nontoxicity, biocompatibility, biodegradability, and the extraordinary ability to self-assemble into a viscous liquid crystalline phase (LCP) in the presence of excess water 21,22 forming a fluid precursor system (FPS). Their use in a gelling system for the development of new formulations has intensified over the last few years in both academic research and industry, mainly for pharmaceutical application.…”

Section: Introductionmentioning

confidence: 99%

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

Nunes

Teixeira

Kaminski

et al. 2016

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

This article reports the development of a precursor liquid crystalline system based on a mixture of monoglycerides (MO) and Cremophor(®) (CREM) that exhibits in situ gelation to a liquid crystalline phase. The effects of different MO/CREM ratios and the water content (WC) on several performance characteristics were investigated with a full factorial design. The formulations were characterized by polarized light microscopy, small-angle X-ray scattering, and water uptake assays. Rheological, syringeability, and mucoadhesion evaluation were also performed. The polarized light microscopy and small-angle X-ray scattering results for average and high MO/CREM ratios (2.1 and 4.0, respectively) indicated the coexistence of phases in transition to the liquid crystalline phase, independently of the WC. These systems became more viscous after taking up water, showing peaks characteristic of a cubic phase. Systems that had average and high MO/CREM ratios also exhibited shear-thinning behavior and high elasticity. Most systems showed suitable mucoadhesion for buccal purposes. Response surface methodology results demonstrated that the relative contribution of MO was the principal factor that affected the performance of the system. Accordingly, these precursor systems with average to high MO/CREM ratios and an average WC (10% w/w) demonstrated physicochemical and mucoadhesive properties that could enable them to be used as an in situ-gelling controlled drug delivery platform.

show abstract

Section: Introductionmentioning

confidence: 99%

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

Nunes

Teixeira

Kaminski

et al. 2016

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

show abstract

“…[82][83][84][85] Mucoadhesion of thermosensitive gels and LCs can be explained by their rheological properties. 39,41,[86][87][88][89][90][91] Moreover, the mucoadhesive force of the liquid crystalline phases is determined by their ability to take up water from the environment. 87 Many theories have attempted to explain the biomucoadhesion; however, for the systems developed, the elastic behavior (G′.G″) has an influence on the bioadhesive process.…”

mentioning

confidence: 99%

Design, characterization, and biological evaluation of curcumin-loaded surfactant-based systems for topical drug delivery

Fonseca-Santos

Santos

Rodero

et al. 2016

IJN

View full text Add to dashboard Cite

From previous studies, it has been found that curcumin exhibits an anti-inflammatory activity and is being used for the treatment of skin disorders; however, it is hydrophobic and has weak penetrating ability, resulting in poor drug transport through the stratum corneum. The aim of this study was to develop liquid crystalline systems for topical administration of curcumin for the treatment of inflammation. These liquid crystalline systems were developed from oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol, and water as the surfactant, oil phase, and aqueous phase, respectively. These systems were characterized, and polarized light microscopy showed anisotropy with lamellar mesophases (Formulation 1) and hexagonal mesophases (Formulations 2 and 3), which were confirmed by the peak ratio measured using small-angle X-ray scattering. In addition, rheological tests revealed that the formulations exhibited gel-like behavior (G′>G″), as evidenced by the increased G′ values that indicate structured systems. Texture profile analysis showed that hexagonal mesophases have high values of hardness, adhesiveness, and compressibility, which indicate structured systems. In vitro studies on bioadhesion revealed that the hexagonal mesophases increased the bioadhesiveness of the systems to the skin of the pig ear. An in vivo inflammation experiment showed that the curcumin-loaded hexagonal mesophase exhibited an anti-inflammatory activity as compared to the positive control (dexamethasone). The results suggest that this system has a potential to be used as a bioadhesive vehicle for the topical administration of curcumin. Therefore, it is possible to conclude that these systems can be used for the optimization of drug delivery systems to the skin.

show abstract

“…Then 8 mL fresh deionized water was added on the surface of the matrix. The weight data were plotted versus time according to mathematic kinetics of first-order and second-order kinetic equations (Souza et al, 2014). The influence of drug solubility, drug loading, proportions of additives (PEG 1000, Tween 80 and gelucire 39/01) on swelling behaviors of SPTSs were investigated.…”

Section: In Vitro Drug Release and Swelling Behavior Of Spts@hard Capmentioning

confidence: 99%

Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs

Zhang

Xiao²,

Huang

et al. 2020

Drug Delivery

View full text Add to dashboard Cite

Smart phase transformation systems@hard capsule (SPTS@hard capsule) based on lyotropic liquid crystalline (LLC) were developed for oral sustained release in this study. Doxycycline hydrochloride (DOXY) and meloxicam (MLX) were used as hydrophilic and hydrophobic model drug, respectively. Two systems were added with different additives, that is, gelucire 39/01, PEG 1000 and Tween 80 to adjust their melting point and release profiles. The phase transformation of these systems could be triggered by water as well as temperature. They could spontaneously transform into cubic phase or hexagonal phase when coming across with water, to achieve the 24 h sustained release profile. In addition, the obtained systems could switch between semisolid state and liquid state when temperature changed within room temperature and body temperature, which facilitated the phase transformation in gastrointestinal tract and during their encapsulation into hard capsules. LLC-based SPTS@hard capsule revealed potential for the industrialization of its oral administration on account of its drugs accommodation with different solubility, controllable release profile and simple preparation process.

show abstract

Mucoadhesive System Formed by Liquid Crystals for Buccal Administration of Poly(Hexamethylene Biguanide) Hydrochloride

Cited by 45 publications

References 60 publications

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

Design, characterization, and biological evaluation of curcumin-loaded surfactant-based systems for topical drug delivery

Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs

Contact Info

Product

Resources

About