Targeted delivery of a poorly water-soluble compound to hair follicles using polymeric nanoparticle suspensions

Pancreatic cancer is the eighth leading cause of cancer death worldwide. For this reason, the development of more effective therapies is a major concern for the scientific community. Accordingly, plants belonging to Plectranthus genus and their isolated compounds, such as Parvifloron D, were found to have cytotoxic and antiproliferative activities. However, Parvifloron D is a very low water-soluble compound. Thus, nanotechnology can be a promising delivery system to enhance drug solubility and targeted delivery. The extraction of Parvifloron D from P. ecklonii was optimized through an acetone ultrasound-assisted method and isolated by Flash-Dry Column Chromatography. Then, its antiproliferative effect was selectivity evaluated against different tumor cell lines (IC50 of 0.15 ± 0.05 μM, 11.9 ± 0.7 μM, 21.6 ± 0.5, 34.3 ± 4.1 μM, 35.1 ± 2.2 μM and 32.1 ± 4.3 μM for BxPC3, PANC-1, Ins1-E, MCF-7, HaCat and Caco-2, respectively). To obtain an optimized stable Parvifloron D pharmaceutical dosage form, albumin nanoparticles were produced through a desolvation method (yield of encapsulation of 91.2%) and characterized in terms of size (165 nm; PI 0.11), zeta potential (−7.88 mV) and morphology. In conclusion, Parvifloron D can be efficiently obtained from P. ecklonii and it has shown selective cytotoxicity to pancreatic cell lines. Parvifloron D nanoencapsulation can be considered as a possible efficient alternative approach in the treatment of pancreatic cancer.

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Synthesis of propylene glycol phospholipids: analogues of α-lecithins and α-cephalins

Canadian Journal of Biochemistry ◽

10.1139/o68-011 ◽

1968 ◽

Vol 46 (1) ◽

pp. 69-74 ◽

Cited By ~ 11

Author(s):

Erich Baer ◽

Angus J. Duke ◽

Dmytro Buchnea

Keyword(s):

Propylene Glycol ◽

Hemolytic Activity ◽

Polyhydric Alcohol ◽

Water Soluble ◽

Asymmetric Center ◽

Water Soluble Compound ◽

Soluble Compound ◽

Dipalmitoyl Lecithin

The synthesis of phospholipids derived from propylene glycol, structurally the least complex polyhydric alcohol to possess an asymmetric center, is described. Representatives of two types of propylene glycol phospholipids were prepared. They are analogues of α-(dipalmitoyl)lecithin and α-(dipalmitoyl)cephalin, and were obtained from D-propylene glycol via the following two series of intermediates: (A) α-trityl D-propylene glycol (I) → α-trityl, β-palmitoyl D-propylene glycol (II) → β-palmitoyl D-propylene glycol (III) → β-palmitoyl D-propylene glycol-α-(phenyl)phosphorylcholine chloride (IV) → β-palmitoyl D-propylene glycol-α-phosphorylcholine (V); and (B) I → II → III → β-palmitoyl D-propylene glycol-α-(phenyl)phosphoryl-N-carbobenzoxyethanolamine (VI) → β-palmitoyl D-propylene glycol-α-phosphorylethanolamine (VII). The palmitoyl D-propylene glycol-α-phosphorylcholine, a highly water-soluble compound, possesses strong hemolytic activity, whereas the palmitoyl D-propylene glycol-α-phosphorylethanolamine has no hemolytic properties whatsoever.

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