Binding of drugs to monoglyceride-based drug delivery systems

Chang, Chin-Ming; Bodmeier, Roland

doi:10.1016/s0378-5173(96)04805-3

Cited by 73 publications

(32 citation statements)

References 10 publications

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“…It was reported that encapsulated molecules such as bupivacaine, lidocaine, and propranole affected the liquid crystalline structure, and under some conditions, these molecules induced a phase transition. [27][28][29] Similarly, results from the current study indicated that the flurbiprofen molecule participated in the stabilizing the hexagonal structure in GME-based LCN system by the interacting with the lipid components and contributed to the formation of hexagonal structure.…”

Section: Fig 2 Small Angle X-ray Diffraction (Saxs) Patterns Of Glysupporting

confidence: 63%

Glyceryl Monooleyl Ether-Based Liquid Crystalline Nanoparticles as a Transdermal Delivery System of Flurbiprofen: Characterization and <i>in Vitro</i> Transport

et al. 2015

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Liquid crystalline nanoparticles (LCNs) were prepared using glyceryl monooleyl ether (GME) by the modified film rehydration method. Hydrogenated lecithin (HL), 1,3-butylene glycol (1,3-BG), and Poloxamer 407 were used as additives. The prepared LCN formulations were evaluated based on particle size, smallangle X-ray diffraction (SAXS) analysis, 1 H-and 19F-NMR spectra, and in vitro skin permeation across Yucatan micropig skin. The composition (weight percent) of the LCN formulations were GME-HL-1,3-BG (4 : 1 : 15), 4% GME-based LCN and GME-HL-1,3-BG (8 : 1 : 15), 8% GME-based LCN and their mean particle sizes were 130-175 nm. Flurbiprofen 5 and 10 mg was loaded into 4% GME-based LCN and 8% GMEbased LCN systems, respectively. The results of SAXS and NMR suggested that both flurbiprofen-loaded formulations consist of particles with reverse type hexagonal phase (formation of hexosome) and flurbiprofen molecules were localized in the lipid domain through interaction of flurbiprofen with the lipid components. Flurbiprofen transport from the LCN systems across the Yucatan micropig skin was increased compared to flurbiprofen in citric buffer (pH 3.0). The 8% GME-based LCN systems was superior to the 4% GME-based LCN for flurbiprofen transport. Since the internal hexagonal phase in the 8% GME-based LCN systems had a higher degree of order compared to the 4% GME-based LCN in SAXS patterns, the 8% GME-based LCN system had a larger surface area, which might influence flurbiprofen permeation. These results indicated that the GME-based LCN system is effective in improving the skin permeation of flurbiprofen across the skin.Key words lyotropic liquid crystal; liquid crystalline nanoparticle; hexosome; skin permeation; flurbiprofen; NMR Under some circumstances, transdermal delivery may be superior to other routes of delivery due to advantages such as avoidance of first pass elimination and a lack of invasiveness. However, relatively few transdermal drugs have been commercialized owing to the efficient barrier function of the stratum corneum, which is located on the outer layer of the skin. To overcome the barrier function of the stratum corneum, several physical and chemical methods have been developed. 1)Recently, lyotropic liquid crystal (LLC) systems have been developed as a chemical method to overcome the stratum corneum barrier.2,3) LLCs are usually composed of amphiphilic molecules and solvents that can form a variety of structures, including lamellar (L α ), hexagonal (normal, or reverse) and inverted cubic (bicontinuous and micellar) structures. 4) Among these LLC systems, some of liquid crystal structures form a liquid crystalline nanoparticles (LCNs) by dispersing in an aqueous environment and the LCNs of reverse hexagonal phase and bicontinuous cubic phase are called "hexosomes (H II )" and "cubosomes," respectively. 3,5) Glycerol monoolate (GMO) has been widely studied as an additive to form LLCs and their LCNs.6,7) Effect of the additives such as block copolymer formation and electrostatic interaction were also i...

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Section: Fig 2 Small Angle X-ray Diffraction (Saxs) Patterns Of Glysupporting

confidence: 63%

Glyceryl Monooleyl Ether-Based Liquid Crystalline Nanoparticles as a Transdermal Delivery System of Flurbiprofen: Characterization and <i>in Vitro</i> Transport

et al. 2015

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“…Included in this category are the newest methods for intravascular delivery, including the use of biodegradable nanoparticles (Schroeder et al, 1998;Song et al, 1997), liposomes (Allen and Moase, 1996; Sakamoto and Ido, 1993), monoglyceride-based systems (Chang et al, 1994), and magnetic microspheres (Chang and Bodmeier, 1997). Many of these novel approaches are evaluating different methods of giving drug-laden molecules that will preferentially accumulate in a tissue, usually combined with selective methods of perfusion, such as i.a.…”

Section: Avant-garde Methods Of Deliverymentioning

confidence: 99%

“…magnetic aminodextran microspheres to RG-2 rat brain tumors and used a magnetic eld to retain the particles within the tumor. They showed that this method resulted in signi cant accumulation of the particles as a result of surface charge and magnetic eld (Chang and Bodmeier, 1997). These methods are too new to be applied to human brain tumors, but are representative of the diverse and novel directions that investigators are using to increase brain tumor delivery.…”

Section: Avant-garde Methods Of Deliverymentioning

confidence: 99%

The blood-brain and blood-tumor barriers: A review of strategies for increasing drug delivery

Groothuis¹

2000

Neuro-Oncol

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Drug delivery to brain tumors has been a controversial subject. Some believe the blood-brain barrier is not important, while others believe it is the major obstacle in treatment and have devised innovative approaches to circumvent it. These approaches can be divided into two categories: those that attempt to increase drug delivery of intravascularly administered drugs by manipulating either the drugs or capillary permeability, and those that attempt to increase drug delivery by local administration. Several strategies have been developed to increase the fraction of intravascular drug reaching the tumor, including intraarterial administration, barrier disruption, new ways of packaging drugs, and, most recently, inhibiting drug ef ux from tumor. When given intravascularly, all drugs have a common drawback: the body acts as a sink, and, even in the best situations, only a small fraction of administered drug actually reaches the tumor. A consequence is that systemic toxicity is usually the dose-limiting factor. When given locally, such as into the cerebrospinal uid or directly into the tumor, 100% of an administered dose is delivered to the target site. However, local delivery is associated with variable and unpredictable spatial distribution and variation in drug concentration. The major dose-limiting factor of most local delivery methods will be neurotoxicity. The relative advantages and disadvantages of the different methods of circumventing the blood-brain barrier are presented in this review, and special attention is given to convection-enhanced delivery, which has particular promise for the local delivery of large therapeutic agents such as monoclonal antibodies, antisense oligonucleotides, or viral vectors. Neuro-Oncology 2, 45-59, 2000 (Posted to Neuro-Oncology [serial online], Doc. 99-30, December 14, 1999 IntroductionThe delivery of drugs to brain tumors has long been a controversial problem. In 1977, Vick et al. wrote in an editorial: "We believe that there is compelling evidence to suggest that the 'blood-brain barrier,' as it is generally conceived, is not one of the factors impeding the success of brain tumor chemotherapy." They went on to say that "dosage, route of administration, tumor cell uptake, metabolic fate within tumor cells, and the washout or sink effect of the extracellular space and CSF are the issues that will have to be studied" (Vick et al., 1977). Some clinicians have agreed with Vick et al. (Donelli et al., 1992;Stewart, 1994); however, on the whole, the belief that the BBB 3 and BTB prevent drugs from reaching brain tumors in suf cient concentrations to kill the tumor cells has motivated numerous attempts to increase the amount of drug that reaches the tumor. Many innovative methods have been used to try to increase drug delivery including, most recently, a method in which drugs are infused directly into brain tumors, a method referred to as convection-enhanced delivery (CED) Laske et al., 1997a;Lieberman et al., 1995). This review Neuro-Oncology n J AN UA RY 2 0 00 45Neuro-Oncology

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“…Therefore, solubilized bioactives in the LLC systems would be released at rates depended on the mesophase structure and type of dissolved solutes [10,13,14]. The electrolytes can also affect the lipids assemblies and structure since they control factors such as curvature, surface area per surfactant, solubilization capacity, susceptibility of the headgroups to solubilization of bioactives, melting, and phase transitions [8,[15][16][17].…”

Section: Introductionmentioning

confidence: 99%

On structural transitions in a discontinuous micellar cubic phase loaded with sodium diclofenac

Efrat

Aserin

Garti

2008

Journal of Colloid and Interface Science

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Binding of drugs to monoglyceride-based drug delivery systems

Cited by 73 publications

References 10 publications

Glyceryl Monooleyl Ether-Based Liquid Crystalline Nanoparticles as a Transdermal Delivery System of Flurbiprofen: Characterization and <i>in Vitro</i> Transport

Glyceryl Monooleyl Ether-Based Liquid Crystalline Nanoparticles as a Transdermal Delivery System of Flurbiprofen: Characterization and <i>in Vitro</i> Transport

The blood-brain and blood-tumor barriers: A review of strategies for increasing drug delivery

On structural transitions in a discontinuous micellar cubic phase loaded with sodium diclofenac

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