Novel Biodegradable Polyester Poly(Propylene Succinate): Synthesis and Application in the Preparation of Solid Dispersions and Nanoparticles of a Water-Soluble Drug

Abstract

Abstract. Poly(propylene succinate) (PPSu) polymers of average molecular weights from 2,800 to 13,100 g/mol were synthesized and characterized with regard to crystallinity, thermal properties, and cytocompatibility. Higher molecular weight samples exhibited lower degree of crystallinity and melted at lower temperatures. Melting of the polymer appeared to begin at 38°C. PPSu cytocompatibility was investigated based on human umbilical vein endothelial cells viability in the presence of increasing concentrations of polymer, and it was found that PPSu exhibited comparable cytocompatibility with poly (DL-lactide). The feasibility of applying PPSu as a drug carrier was shown for the first time, as solid dispersions and nanoparticles of sodium fluvastatin based in PPSu were prepared. Drug release rates decreased with increasing the molecular weight of PPSu in both solid dispersions and nanoparticles. For dispersions prepared from PPSu of the same molecular weight, drug release rates increased with drug loading. It appears that PPSu applicability as a drug carrier warrants further consideration.

Synthesis of folate- pegylated polyester nanoparticles encapsulating ixabepilone for targeting folate receptor overexpressing breast cancer cells

“…4). Neat PPSu exhibited a melting point at 49°C and a T g value at -27.6°C, in accordance to our previous work [8]. The addition of MAL-PEG into PPSu reduced the melting point of PPSu to 35.6°C due to cocrystallization with PEG, as was verified by the XRD studies, while a second melting point appeared at 47.4°C.…”

“…Although these polyesters are widely used as drug carriers and implants, their low degradation rate [6] sparked an increased interest for the synthesis of new materials with innovative and enhanced properties. Poly(propylene succinate) (PPSu) is such a new biocompatible polyester with relatively high biodegradation rate due to its low degree of crystallinity [7,8]. Furthermore, due to its low melting point (T m = 44°C), which is close to the physiological body temperature [9,10], PPSu could be used as drug nanocarrier appropriate for selective drug release at the tumor site using local hyperthermia.…”

Slow relaxations in semicrystalline poly(butylene succinate) below and aboveTg

“…In fact, the pellets have been prepared at 145 C (above the melting temperature), dried under vacuum at 100 C (above the crystallization temperature), and cooled very slowly inside the vacuum oven down to room temperature, so that the crystallization temperature region was crossed at rates <1 C min 21 . The crystallization was thus complete, as the article by Bikiaris et al [12] stated that PBS crystallizes rapidly on cooling from the melt, which is confirmed by our thermogram shown below in Figure 2. Furthermore, the TSDC experiments covered the temperature interval between 2130 and 25 C, well below the crystallization temperature.…”

The role of the carrier in the formulation of pharmaceutical solid dispersions. Part I: crystalline and semi-crystalline carriers

“…Semicrystalline carriers that have been applied in the formulation of pharmaceutical solid dispersions so far are PEG and its surface active derivatives such as poloxamer [58,59], gelucire [60,61] as well as some less commonly used polymers including chitosan and [62] poly(propylene succinate) [63]. These carriers contain both crystalline and amorphous domains, the proportions of which depend on the molecular weight of the carrier and the sample preparation conditions.…”