Effect of Polyvinyl Pyrrolidone on the Thermal Phase Transition of 1,2 Dipalmitoyl-sn-glycero-3-phosphocholine Bilayer

Savva, Michalakis; Torchilin, Vladimir P.; Huang, Leaf

doi:10.1006/jcis.1999.6343

Cited by 26 publications

(31 citation statements)

References 15 publications

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“…[31][32][33] Incorporation of PVP within a DPPC lipid film promotes interaction with the DPPC acyl chains and consequently, liposome incorporation. 34 Therefore, we speculate that a similar interaction occurred, with POPC integrating PVP within our liposomes. Thus, the chosen polymers may help to maintain the structural conformation of liposomal nanoparticles and may improve stability.…”

mentioning

confidence: 57%

Liposomal nanoparticles encapsulating iloprost exhibit enhanced vasodilation in pulmonary arteries

Jain¹,

Leber²,

Nagaraj³

et al. 2014

IJN

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Prostacyclin analogues are standard therapeutic options for vasoconstrictive diseases, including pulmonary hypertension and Raynaud’s phenomenon. Although effective, these treatment strategies are expensive and have several side effects. To improve drug efficiency, we tested liposomal nanoparticles as carrier systems. In this study, we synthesized liposomal nanoparticles tailored for the prostacyclin analogue iloprost and evaluated their pharmacologic efficacy on mouse intrapulmonary arteries, using a wire myograph. The use of cationic lipids, stearylamine, or 1,2-di-(9Z-octadecenoyl)-3-trimethylammonium-propane (DOTAP) in liposomes promoted iloprost encapsulation to at least 50%. The addition of cholesterol modestly reduced iloprost encapsulation. The liposomal nanoparticle formulations were tested for toxicity and pharmacologic efficacy in vivo and ex vivo, respectively. The liposomes did not affect the viability of human pulmonary artery smooth muscle cells. Compared with an equivalent concentration of free iloprost, four out of the six polymer-coated liposomal formulations exhibited significantly enhanced vasodilation of mouse pulmonary arteries. Iloprost that was encapsulated in liposomes containing the polymer polyethylene glycol exhibited concentration-dependent relaxation of arteries. Strikingly, half the concentration of iloprost in liposomes elicited similar pharmacologic efficacy as nonencapsulated iloprost. Cationic liposomes can encapsulate iloprost with high efficacy and can serve as potential iloprost carriers to improve its therapeutic efficacy.

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mentioning

confidence: 57%

Liposomal nanoparticles encapsulating iloprost exhibit enhanced vasodilation in pulmonary arteries

Jain¹,

Leber²,

Nagaraj³

et al. 2014

IJN

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“…In a recent investigation, we found that PVP homopolymer interacts with the phospholipid bilayer causing the DPPC main phase transition to move to lower temperatures (12). Torchilin and co-workers have shown that blood clearance of liposomes protected by PVP-PE was much faster than that of liposomes protected by PEG-PE (8).…”

Section: Discussionmentioning

confidence: 97%

“…The procedure has been described elsewhere (12). Briefly, DSC scans were performed on a MC-2 Microcal high sensitivity calorimeter (Microcal, Inc., Northampton, MA) at a heating rate of 0.5, 0.75, or 1°C/min.…”

Section: Calorimetrymentioning

confidence: 99%

Effect of Grafted Amphiphilic PVP–Palmityl Polymers on the Thermotropic Phase Behavior of 1,2 Dipalmitoyl- sn-glycero-3-phosphocholine Bilayer

Savva

Torchilin

Huang

1999

Journal of Colloid and Interface Science

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“…Enhancement of drug dissolution rate is caused by the inhibition of crystallization of drug and formation of high free-energy amorphous phase on core pellets during the coating process. This is mostly offered by anti-plasticizing effect of PVP and by PVPs surface adsorption and efficient steric hindrance for nucleation and crystal growth 27,28 . In comparison to SDs with PVP, formulations containing cPVP showed a weaker solubilization effect.…”

Section: In Vitro Drug Release Studymentioning

confidence: 99%

Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate

Kolašinac¹,

Kachrimanis²,

Djuriš³

et al. 2012

Drug Development and Industrial Pharmacy

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Solid dispersion systems have been widely used to enhance dissolution rate and oral bioavailability of poorly water-soluble drugs. However, the formulation process development and scale-up present a number of difficulties which has greatly limited their commercial applications. In this study, solid dispersions (SDs) of desloratadine (DSL) with povidone (PVP) and crospovidone (cPVP) were prepared by spray coating technique. The process involved the spray application of 96% ethanol solution of DSL and PVP/cPVP, and subsequent deposition of the coprecipitates onto microcrystalline cellulose pellets during drying by air flow in a mini spray coater. The results from the present study demonstrated that the spray coating process is efficient in preparing SDs with enhanced drug dissolution rate and it is highly efficient in organic solvent removal. Both PVP and cPVP greatly improved drug dissolution rate by SDs, with PVP showing better solubilization capability. Very fast drug dissolution rate is achieved from SDs containing PVP regardless of differences in K grade. SD with smaller particles of cPVP have higher drug dissolution rate in comparison to the cPVP with larger particles. Results from physical state characterization indicate that DSL in SDs exist in the amorphous (high free-energy) state which is probably stabilized by PVP/cPVP. After 6-month accelerated stability study, DSL remains amorphous, while PVP and cPVP act as anti-plasticizing agents, offering efficient steric hindrance for nucleation and crystal growth.

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Effect of Polyvinyl Pyrrolidone on the Thermal Phase Transition of 1,2 Dipalmitoyl-sn-glycero-3-phosphocholine Bilayer

Cited by 26 publications

References 15 publications

Liposomal nanoparticles encapsulating iloprost exhibit enhanced vasodilation in pulmonary arteries

Liposomal nanoparticles encapsulating iloprost exhibit enhanced vasodilation in pulmonary arteries

Effect of Grafted Amphiphilic PVP–Palmityl Polymers on the Thermotropic Phase Behavior of 1,2 Dipalmitoyl- sn-glycero-3-phosphocholine Bilayer

Spray coating as a powerful technique in preparation of solid dispersions with enhanced desloratadine dissolution rate

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