Influence of the leprosy drug, dapsone on the model membrane dipalmitoyl phosphatidylethanolamine

Panicker, Lata

doi:10.1016/j.tca.2006.05.007

Cited by 6 publications

(3 citation statements)

References 26 publications

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“…The transition enthalpy, ÁH LC of the subgel, L LC phase is approximately 3 kJ mol À1 [37]. However, the gel phase of DPPE-buffer pH 7.4 system did not form subgel L LC and/or L HC phases and the heating thermograms did not show any significant change when compared to e % 0 scans.…”

Section: 1mentioning

confidence: 88%

Interaction of keratolytic drug, salicylic acid with dipalmitoyl phosphatidylethanolamine vesicles

2008

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Salicylic acid (SA), a keratolytic drug, is used to treat skin disorder like corns, warts, and acne. To understand the mechanism by which SA interacts with the cell membranes, we have investigated its interaction with dipalmitoyl phosphatidylethanolamine (DPPE) vesicles using DSC, 1 H NMR and Raman spectroscopy. Presence of drug asymmetrically broadened the acyl chain melting transition and shifted the transition temperature, T m , to lower value. Both, NMR and DSC studies indicate that the drug molecules are located in the glycerol backbone region of the lipid bilayer and increase the membrane headgroup fluidity. At high drug concentration, additional transitions are observed whose intensity increases with increasing drug concentration. In cholesterol doped DPPE dispersion the interaction of SA with DPPE bilayer is more. The transformation of the gel phase of DPPE dispersion to a stable crystalline subgel phase(s) is accelerated by the presence of SA.

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Section: 1mentioning

confidence: 88%

Interaction of keratolytic drug, salicylic acid with dipalmitoyl phosphatidylethanolamine vesicles

2008

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“…This behavior is similar to that reported in model lipidic membranes, in which the peptide is considered as a "defect" in the lipid bilayer, which can be randomly distributed in the hydrocarbon region, affecting lipid interactions due to the electrostatic charges and to the geometry of the guest molecule. 34,35 An immediate release was observed ( Figure 5); 99.60% of CyA was released from the SLN at 45 min, indicating the presence of an amorphous structure of the lipid and maybe the existence of CyA molecules on the NP surface, which allows a rapid dissolution and possibly higher loadings.…”

Section: Discussionmentioning

confidence: 98%

Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method

Urbán-Morlán

Ganem-Rondero²,

Melgoza-Contreras³

et al. 2010

IJN

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Solid lipid nanoparticles (SLNs) have been used for carrying different therapeutic agents because they improve absorption and bioavailability. The aim of the study was to prepare lipidic nanoparticles containing cyclosporine (CyA) by the emulsification-diffusion method and to study their physicochemical stability. . Systems with Gelucire ® were characterized by particle size, Z-potential, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), entrapment efficiency and in vitro release. Particle size and Z-potential were evaluated for at least three months. With a high CyA content ($60 mg) in Gelucire  SLNs, variations in size were greater and particle size also increased over time in all batches; this effect may have been caused by a probable expulsion of the drug due to the lipid's partial rearrangement. While the Z-potential decreased 10 mV after three months, this effect may be explained by the superficial properties of the drug that make the molecules to be preferably oriented at the solid-liquid interface, causing a change in the net charge of the particle. SEM confirmed size and shape of the nanoparticles. DSC studies evidenced that CyA affects the lipid structure by a mechanism still unknown. The entrapment efficiency was higher than 92%, and CyA release from SLNs was relatively fast (99.60% in 45 min).

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“…It is noteworthy the different formulations described in Tables II and IV present different active ingredient concentrations. This may also be a source of variability as, for instance, the molecule of DAP has shown to intercalate the polar groups of phospholipids and increase membrane fluidity (138).…”

Section: Overview and Future Perspectivesmentioning

confidence: 99%

Emerging Technologies to Target Drug Delivery to the Skin – the Role of Crystals and Carrier-Based Systems in the Case Study of Dapsone

2020

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Dapsone (DAP) is a long-established molecule that remains a promising therapeutic agent for various diseases mainly because it combines antimicrobial and antiinflammatory activities. Its oral application, however, is limited by the dose-dependent hematological side effects that may rise from systemic exposure. As an alternative to overcome this limitation, the administration of DAP to the skin has witnessed prominent interest in the past 20 years, particularly when applied to the treatment of dermatological disorders. In this review, all technological strategies proposed to the topical delivery of DAP are presented. Most of the reported studies have been devoted to the clinical use and safety of a gel formulation containing both solubilized and microcrystalline drug, however, the technological characteristics of such preparation are still missing. In parallel, the incorporation of DAP into vesicular and particulate carriers (e.g. nano-and microemulsions, niosomes, invasomes, bilosomes, cubosomes, solid lipid nanoparticles, nanostructured lipid carriers, polymeric nanocapsules and polymer-lipid-polymer hybrid nanoparticles) appears to be an alternative to provide greater drug release control, enhanced drug solubilization and follicular targeting. Indeed, the main application of DAP topical formulations reported in the literature was the treatment of acne vulgaris, a disease located in the hair follicle. Other diseases affecting different regions of the skin (e.g. cutaneous lupus erythematosus and cutaneous leishmaniasis), however, may also benefit from a topical therapeutic regimen containing DAP. Therefore, the investigation of appendageal route in comparison to passive transmembrane diffusion as a function of targeted disease, as well as pharmacokinetic studies, are perspectives highlighted herein. Such studies may drive future efforts towards the rational development of safe and effective technologies to deliver DAP to the skin.

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Influence of the leprosy drug, dapsone on the model membrane dipalmitoyl phosphatidylethanolamine

Cited by 6 publications

References 26 publications

Interaction of keratolytic drug, salicylic acid with dipalmitoyl phosphatidylethanolamine vesicles

Interaction of keratolytic drug, salicylic acid with dipalmitoyl phosphatidylethanolamine vesicles

Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method

Emerging Technologies to Target Drug Delivery to the Skin – the Role of Crystals and Carrier-Based Systems in the Case Study of Dapsone

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