Low viscosity monoglyceride-based drug delivery systems transforming into a highly viscous cubic phase

Chang, Chin-Ming; Bodmeier, Roland

doi:10.1016/s0378-5173(98)00180-x

Cited by 87 publications

(45 citation statements)

References 10 publications

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“…The cubic phase gel was transparent but stiff and viscous which limited its potential use as the delivery system (17). However, lower viscous cubic phase gel could be obtained by adding organic solvents (e.g., propylene glycol (PG), ethanol, polyethylene glycol, and N-methyl-2-pyrrolidone) (18,19). In this study, the MO-PG-water was selected to investigate the cubic phase system based on the following two reasons: first, PG could decrease the cubic phase gel viscosity and second, PG was a well-known skin penetration enhancer and used as a common additive in topical formulations.…”

Section: Introductionmentioning

confidence: 99%

Design and In Vitro Evaluation of Capsaicin Transdermal Controlled Release Cubic Phase Gels

et al. 2010

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Abstract. The purpose of this study was to design and investigate the transdermal controlled release cubic phase gels containing capsaicin using glycerol monooleate (MO), propylene glycol (1,2-propanediol, PG), and water. Three types of cubic phase gels were designed based on the ternary phase diagram of the MO-PG-water system, and their internal structures were confirmed by polarizing light microscopy (PLM) and small-angle X-ray scattering (SAXS). Release results showed the cubic phase gels could provide a sustained system for capsaicin, while the initial water content in the gels was the major factor affecting the release rate. Release kinetics was determined to fit Higuchi's square-root equation indicating that the release was under diffusion control. The calculated diffusion exponent showed the release from cubic phase gels was anomalous transport. The unique structure of the cubic phases, capsaicin distributed in the lipid bilayers, and cubic phase gel swelling contributed to the release mechanism. The cubic phase gel may be an interesting application for transdermal delivery system of capsaicin in alleviating the post-incision pain.

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Section: Introductionmentioning

confidence: 99%

Design and In Vitro Evaluation of Capsaicin Transdermal Controlled Release Cubic Phase Gels

et al. 2010

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“…The identification of the liquid crystalline phases formed using monoolein/water systems in the presence of drugs is fundamental to the development of drug delivery systems based on liquid crystals because the structure of the mesophase presented by the system can influence drug release. The addition of drugs or additives to liquid crystalline systems can modify the phase structures and system properties, which may influence drug release profiles (20,21,26,34,35). Several authors have reported altered properties in the liquid crystalline phase of monoolein/water systems due to the addition of drugs and solvents (18,20,25,34,(36)(37)(38)(39).…”

Section: Discussionmentioning

confidence: 99%

“…The addition of drugs or additives to liquid crystalline systems can modify the phase structures and system properties, which may influence drug release profiles (20,21,26,34,35). Several authors have reported altered properties in the liquid crystalline phase of monoolein/water systems due to the addition of drugs and solvents (18,20,25,34,(36)(37)(38)(39). The presence of a drug can affect the curvature of the lipid bilayer and change the average area of the lipid head group, which changes monoglyceride molecular packing and promotes a phase transition (18,23).…”

Section: Discussionmentioning

confidence: 99%

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

et al. 2014

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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.

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“…Their ability to control the release of drugs and their excellent biocompatibility make liquid crystals based on polar lipids such as monoolein (MO) particularly attractive as delivery matrices for the topical and transdermal delivery of drugs [20,[22][23][24][25], including prodrugs and photosensitizers in PDT for skin cancer [13,14]. Moreover, liquid crystalline lipid-water phases with an inverse structure (reverse hexagonal and the cubic phases) can co-exist in equilibrium with an excess of water, forming kinetically stable colloidal dispersions [26].…”

Section: Introductionmentioning

confidence: 99%

“…In contrast, the water-soluble zinc phthalocyanine tetrasulfonate (ZnPcSO 4 ) has displayed high photodynamic efficiency and reduced phototoxic side effects in the treatment of brain and ocular tumors [18]. However, with exception of a few studies [19][20][21], there is a lack of data on the application of ZnPcSO 4 in PDT for skin cancer.Their ability to control the release of drugs and their excellent biocompatibility make liquid crystals based on polar lipids such as monoolein (MO) particularly attractive as delivery matrices for the topical and transdermal delivery of drugs [20,[22][23][24][25], including prodrugs and photosensitizers in PDT for skin cancer [13,14]. Moreover, liquid crystalline lipid-water phases with an inverse structure (reverse hexagonal and the cubic phases) can co-exist in equilibrium with an excess of water, forming kinetically stable colloidal dispersions [26].…”

mentioning

confidence: 99%

Liquid Crystal Nanodispersions Enable the Cutaneous Delivery of Photosensitizer for Topical PDT: Fluorescence Microscopy Study of Skin Penetration

Praça¹,

Medina²,

Petrilli³

et al. 2012

CNANO

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Topical photodynamic therapy (PDT) has been applied to almost all types of nonmelanoma skin cancer and numerous superficial benign skin disorders. Strategies to improve the accumulation of photosensitizer in the skin have been studied in recent years. Although the hydrophilic phthalocyanine zinc compound, zinc phthalocyanine tetrasulfonate (ZnPcSO4) has shown high photodynamic efficiency and reduced phototoxic side effects in the treatment of brain tumors and eye conditions, its use in topical skin treatment is currently limited by its poor skin penetration. In this study, nanodispersions of monoolein (MO)-based liquid crystalline phases were studied for their ability to increase ZnPcSO4 uptake by the skin. Lamellar, hexagonal and cubic crystalline phases were prepared and identified by polarizing light microscopy, and the nanodispersions were analyzed by dynamic light scattering. In vitro skin penetration studies were performed using a Franz's cell apparatus, and the skin uptake was evaluated in vivo in hairless mice. Aqueous dispersions of cubic and hexagonal phases showed particles of nanometer size, approximately 224 ±10 nm and 188 ± 10 nm, respectively. In vitro skin retention experiments revealed higher fluorescence from the ZnPcSO4 in deeper skin layers when this photosensitizer was loaded in the hexagonal nanodispersion system when compared to both the cubic phase nanoparticles and the bulk crystalline phases (lamellar, cubic and hexagonal). The hexagonal nanodispersion showed a similar penetration behavior in animal tests. These results are important findings, suggesting the development of MO liquid crystal nanodispersions as potential delivery systems to enhance the efficacy of topical PDT.Keywords: Liquid crystalline phases, nanodispersion, skin cancer, skin penetration, photodynamic therapy, zinc phthalocyanine. INTRODUCTIONTopical photodynamic therapy (PDT) has been applied to almost every type of superficial nonmelanoma skin cancer and numerous benign skin disorders [1][2]. PDT is based on the administration of a photosensitizing drug and its selective retention in malignant tissue and its subsequent activation by light at specific wavelengths, causing cell death by the production of free radicals and/or reactive oxygen species [3,4]. Numerous strategies have been studied in recent years in attempts to improve the accumulation of photosensitizers and their precursors in the skin, including the use of microemulsions [5] [13][14][15]. Lipophilic phthalocyanines (e.g., zinc and chloroaluminum compounds) have been widely used as photosensitizers in preclinical studies of PDT for the treatment of skin cancer [16,17]. In contrast, the water-soluble zinc phthalocyanine tetrasulfonate (ZnPcSO 4 ) has displayed high photodynamic efficiency and reduced phototoxic side effects in the treatment of brain and ocular tumors [18]. However, with exception of a few studies [19][20][21], there is a lack of data on the application of ZnPcSO 4 in PDT for skin cancer.Their ability to control the release of dru...

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Low viscosity monoglyceride-based drug delivery systems transforming into a highly viscous cubic phase

Cited by 87 publications

References 10 publications

Design and In Vitro Evaluation of Capsaicin Transdermal Controlled Release Cubic Phase Gels

Design and In Vitro Evaluation of Capsaicin Transdermal Controlled Release Cubic Phase Gels

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

Liquid Crystal Nanodispersions Enable the Cutaneous Delivery of Photosensitizer for Topical PDT: Fluorescence Microscopy Study of Skin Penetration

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