• Archives of Pharmacal Research
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• v.18 no.1
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• pp.18-21
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• 1995

Poly(ethylene glycol)(PEG) macrocers teminated with acrylate groups and semi-interpenetrating polymer networks (IPNs) composed of poly-.epsilon.-capolactone(PCL) and PEG macromer were syntheswized with the aim of obtaining a bioerodible hydrogel that could be used to release drugs for implantable delivery system. Polymerization of PEG macromer resulted in the formation of cross-linked gels due to the multifunctionality of macromer. Non-crosslinked PCL chains were interpenetrated into the cross-linked three-dimensions networks of PEG. The IPNs, largw drug loading lower concentration of PEG macromer in the IPNs concentration and the higher molecular weight of PEG macromer. Also, 5-FU was more fast released than hydrocortisone to the increased water solubility.

• Archives of Pharmacal Research
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• v.9 no.2
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• pp.63-73
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• 1986

The use of biodegradable polymetric materials as drug carriers is a relatively new dimension in polymeric drug delivery systems. A number of biodegradable or bioerodible polymers, such as poly(lactic/glycolic acid) copolymer, poly($\alpha$-amino acid), polyanhydride, and poly (ortho ester) are currently being investigated for this purpose. These polymers are useful for matrix and reservoir-type delivery devices. In addition, when chemical functional groups are introduced to the biodegradable polymer backdone, such as poly (N-(2-hydroxypropyl) methacrylamide), the therapeutic agent can be covalently bound directly or via spacer to the backbone polymer. These polymer/drug conjugates represent another new dimension in biodegradable polymeric drug delivery systems. In addition, examples of biodegradable polymeric durg delivery systems currently being investigated will be discussed for the purpose of demonstrarting the potential importance of this new field.

• Journal of Pharmaceutical Investigation
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• v.29 no.1
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• pp.21-27
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• 1999

Semi-solid poly(ortho esters) (POE) were prepared to provide bioerodible carriers for sustained drug delivery systems of naloxone (NLX) in the treatment of narcotic addiction. As the POE have viscous behavior at room temperature, a significant advantage of this polymer is that it can be injected without any surgical intervention. The POE was synthesized by a transesterification reaction between 1,2,6-hexanetriol and trimethyl orthoacetate, and the structure of the polymer was confirmed by IR. The in vitro release of the drug from POE was studied. The release rate of NLX decreased with increasing intrinsic viscosities of the polymer. In vivo biocompatibility studies were carried out in rats with NLX loaded POE. Histopathological analysis showed that NLX implants are well-tolerated by rats when used subcutaneously. Pharmacokinetic studies of POE-NLX implants of two different viscosities were carried out in rabbits. In all cases, plasma concentrations of NLX were maintained over 1 ng/ml for at least 168 hours, but initial burst effect was observed. Mean residence time(MRT) was found to depend on the viscosity of the polymer.

• Journal of Pharmaceutical Investigation
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• v.29 no.2
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• pp.93-98
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• 1999

Semi-solid poly(ortho esters) (POE) were prepared to provide bioerodible carriers for sustained drug delivery systems of nifedipine in the treatment of cardiovascular disease. As the POE has viscous behavior at room temperature, a significant advantage of this polymer is that it can be injected without any surgical intervention. The POE was synthesized by a transesterification reaction between 1,2,6-hexanetriol and trimethyl orthoacetate and the nifedipine release from POE was studied in vitro. The release rate of nifedipine decreased with increasing the amount of nifedipine and the diethanolamine dispersed in the polymer. But the excess amounts, above 3%, of diethanolamine retarded the release of nifedipine. In vivo biocompatibility studies were carried out in rats with nifedipine loaded POE. Histopathological analysis showed that nifedipine loaded POE implants were well-tolerated by rats when used subcutaneously. In case of the rats implanted POE containing diethanolamine, tissue necrosis and inflammation were occured. Pharmacokinetic studies of nifedipine loaded POE implants were carried out in rabbits. In all cases, plasma concentrations of nifedipine were maintained over 15 ng/ml for at least 360 hours and biological half $life(t_{1/2})$ and mean residence time(MRT) were increased by addition of diethanolamine.

• Journal of Veterinary Clinics
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• v.19 no.2
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• pp.228-235
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• 2002

Mastitis is the most costly disease results in lost milk production, decreased milk quality, milk discard, early culling of cows, drug costs and labor costs in dairy cow. Until now, a antibiotic administration at the end of lactation, dry cow therapy has been known the most effective and widely used mastitis control method. However, dry cow therapy do not control a new infection in the late dry and prepartum period because dry cow products have only persistent activity in the early dry period. Therefore, this study was conducted to evaluate clinical effect of sustained released biodegradable cephalexin microsphere using PLGA in bovine mastitis control during dry period. PLGA has been approved as controlled drug release system because of non-toxic, non-tissue reactive and bioerodible characteristics. This study revealed that cephalexin microsphere had a spherical shape with characteristic porous structure on the surface. Also, in vitro drug release studies are clearly observed that the release rate of cephalexin from PLGA microsphere decrease during the first 21 days after initial burst and then increase again between 3 and 4 weeks showing pulsatile releasing pattern. On the other hand, as tried in field the new infection rate, cure rate and mean SCC after parturition in cephalexin microsphere infused group were significantly differenced as compared to the control group. Accordingly, a sustained release of cephalexin from a biodegradable microsphere could make dry cow therapy more efficiently by preventing a new infection and decreasing the number of existing infection of mammary gland during dry period.