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Thermosensitive micelles composed of a copolymer of methoxy polyethylene glycol (mPEG), polylactic acid (PLA), and 1,6-bis (p-carboxyphenoxy) hexane (CPH), namely methoxy polyethylene glycol-co-polylactic acid-co-aromatic anhydride (mPEG-PLCPHA), were fabricated for application as a promising hydrophilic drug carrier. The copolymer can self-assemble into micelles in PBS by hydrophobic interaction. The diameters of these micelles increased as the environmental temperature increased. An increase in viscosity with sol-to-gel transition occurred as temperature increased from room temperature to body temperature. During the in vitro degradation process, hydrogels demonstrated a more stable degradation rate. Both in vitro and in vivo cytotoxicity results showed that the materials had excellent biocompatibility due to less acidic products formation. In vitro cefazolin release profiles showed a stable release for 30 days. The hydrogel encapsulated cefazolin exhibited a good antibacterial effect. Based on these results, mPEG-PLCPHA can serve as an injectable depot gel for drug delivery., From the Clinical Editor: In this study, thermosensitive hydrogel encapsulated cefazolin was found to exhibit good antibacterial effects with sustained levels for up to 30 days, enabling the development of an injectable depot gel for long-term drug delivery., (© 2013.)

A novel biomaterial: poly(sebacic anhydride-co-ethylene glycol) was synthesized by introducing poly(ethylene glycol) (PEG) into a polyanhydride system. This copolymer was synthesized using sebacic acid and PEG via melt-condensation polymerization. The crystalline behavior of these synthesized products was studied, and compared to that of polymer blends of poly(sebacic anhydride) (PSA) and PEG. The crystallinity of PSA chain segments can be significantly enhanced by increasing chain mobility via the introduction of PEG. The crystallinity of the PSA component in copolymers was substantially greater than that of blends. However, the crystalline growth of the PEG segments was totally hindered by the presence of PSA chain segments, such that no crystal for PEG component was found in these copolymers. Besides, a dynamic mechanical analysis of these materials was also performed to provide additional information concerning visco-elastic behavior for other biomedical applications, where it was found that the viscous behavior in copolymers was more significant than in neat PSA and PEG., (Copyright 2002 Elsevier Science Ltd.)

Abstract: Background/Purpose: Durable mechanical strength and biocompatibility are the two major requirements for osteogenic scaffolds. Polyanhydrides are a class of biodegradable polymers characterized by anhydride bonds that connect repeating units of the polymer backbone chain. Hydroxyapatite (HAP) is the main component of human bone and is a good osteoinductive factor that promotes bone mineralization. This work validates the combination of polyanhydrides and HAP for biomedical application. Methods: Polyanhydride copolymers were fabricated from sebacic acid (SA) and 1,6-bis(p-carboxyphenoxy)hexane (CPH). HAP was surface-modified by polycaprolactone (PCL), and testing tablets were made using different ratios of copolymers and surface-grafted HAP (g-HAP). Degradation tests were performed to evaluate mechanical strength, pH, and weight loss. Biocompatibility was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and live/dead stain test. Cell affinity was measured using scanning electronic microscopy (SEM). Results: The favorable surface erosion property of polyanhydrides prevented marked changes in the mechanical properties over time. In addition, the degradation byproducts of the copolymer did not cause a serious decline in pH and were less harmful to the cells. g-HAP increased cell affinity for the polymer surface. Conclusion: The research team synthesized polyanhydride/g-HAP composites with high mechanical strength, slow degradation, and excellent biocompatibility. The result showed that a CPH/SA ratio of 7:3 in combination with 10 wt% g-HAP was optimal as bone substitute. [Copyright &y& Elsevier]

Suitable carrier systems for sustained release of curcumin were studied by using the self-assembled polymeric micelles. Poly(ethylene glycol) methyl ether and poly(aromatic anhydride) were used as the hydrophilic and hydrophobic blocks, respectively, in forming amphiphilic diblock copolymers. Four different types of polymers methoxy poly(ethylene glycol- b-1,3-bis( p-carboxyphenoxy)propane) (mPEG [ABSTRACT FROM AUTHOR]

Abstract: Poly(sebacic anhydride-co-ethylene glycol) was synthesized by using sebacic anhydride prepolymer and poly(ethylene glycol) for encapsulation of p-nitroaniline and brilliant blue G as modeling drugs to investigate the behavior of hydrophobic and hydrophilic drug release, respectively. Since p-nitroaniline is likely located in the sebacic anhydride-rich phase and brilliant blue G in the PEG-rich phase, respectively, their incorporation would affect the phase behavior of the host polymer. Different pore structure of eroded polymer matrix and drug release behavior were identified for hydrophobic and hydrophilic compounds. With a certain amount of PEG in the copolymer matrix, low drug release rate was accomplished for hydrophobic drug incorporation. [Copyright &y& Elsevier]

In this research, poly(sebacic anhydride) was synthesized via melt-condensation. The polymer was then blended with poly(ethylene glycol) in various ratios by solvent casting, to obtain the desired polymer blends. A differential scanning calorimeter was employed to investigate the crystalline behavior of the blends. Blends with under 10% poly(ethylene glycol) were found to consist of two partially miscible polymers in the amorphous phase. This compatibility of the two polymers may induce the crystallization of the poly(sebacic anhydride) component from decreasing the glass transition temperature of the poly(sebacic anhydride) component in the blending system due to the presence of poly(ethylene glycol) chain segments. Furthermore, phase separation occurred and the crystallinity of poly(sebacic anhydride) diminished when at least 20% poly(ethylene glycol) was present in the blends. These results were verified by the variation in the absorptions of carbonyl groups in infrared spectra; these spectra exhibit the changes in crystallinity of poly(sebacic anhydride) in the blends. [Copyright &y& Elsevier]

A system for localized drug delivery composed of polyanhydride polymers was studied. The polymers were made via melt-condensation of sebacic acid (SA) with different amount of 1, 3-bis (p-carboxyphenoxy) propane (CPP) as copolymers. By double emulsion technique, microspheres with core/shell-like structure were fabricated. Hydrophilic compound Brilliant Blue G (BBG) was encapsulated in the inner core(s) region with loading efficiencies of 50% ~ 60% for poly (SA) and 40% ~ 45% for poly(SA-CPP) copolymer. Hydrophobic compound, curcumin, was encapsulated in the outer shell region at efficiencies about 90%. Drug release profiles show no initial burst and stable release rates. The studied delivery system was showed to provide stable release for both hydrophilic and hydrophobic compounds simultaneously. [ABSTRACT FROM AUTHOR]

Poly (1,6-bis- ( p -carboxyphenoxy hexane)- co - (sebacic anhydride)) (PANH), is a polyanhydride copolymer which has good biocompatibility, and degrades to non-toxic products with a predictable rate of degradation. Nano-sized hydroxyapatite (HAP) is a well-known biomaterial which has been applied in bone regeneration due to its osteoconductivity. However, nano-sized HAP has poor colloidal stability which leads to agglomeration when incorporated into polymeric composites. In this work we describe the surface grafting of poly(ɛ-caprolactone) to HAP (PCL-gHAP) to improve the interfacial adhesion and dispersion of HAP particles in a PANH matrix to form a composite material. The use of scanning electron microscopy-backscattered electron (SEM-BSE) detector and the combination of focused ion beam (FIB)/ transmission electron microscopy (TEM) provided a powerful approach for observing the dispersion of HAP particles in the polymer matrix. We show that surface modification of HAP with PCL improved the homogeneity of the dispersion of HAP particles in the composites and affected the composite morphology during hydrolytic degradation. Composites with high HAP content displayed high compressive strength and a fast rate of degradation. The PCL-gHAP/PANH composites showed superior maintenance of mechanical properties compared with HAP/PANH composites during degradation. A preliminary in vivo study on rat calvaria repair, demonstrated the superior performance of PCL-gHAP/PANH composites. The results suggest that the newly developed PCL-gHAP/PANH composite materials have great potential of serving as a new substrate for bone tissue engineering. [ABSTRACT FROM AUTHOR]

Abstract: In this study, a biodegradable in situ gel-forming controlled drug delivery system based on a thermosensitive methoxy polyethylene glycol-co-poly (lactic acid-co-aromatic anhydride) (mPEG-PLCPPA) hydrogel was studied. The hydrogels were formed by micelle aggregation with rising temperature. The hydrogels underwent a temperature-dependent sol–gel–sol transition, which was a flowing sol at ambient temperature and a non-flowing gel at the physiological body temperature. The residual weight and pH value changes after degradation and the viscosity properties of the hydrogel were investigated. The in vitro release behavior of vancomycin from the mPEG-PLCPPA hydrogels at different concentrations was also investigated. The results showed that the mPEG-PLCPPA amphiphilic copolymer could self-assemble to form micelles at low concentrations, and that the particle sizes gradually increased with increasing temperature. The hydrogel maintained a stable degradation rate and provided a moderate pH microenvironment after degradation for 30 days. Vancomycin sustained a stable release profile from the hydrogel over a 10-day period. Furthermore, good biocompatibility was proven by MTT assay and live and dead test. Therefore, the mPEG-PLCPPA hydrogel shows promise as an injectable local antibiotic delivery system. [Copyright &y& Elsevier]