• Title/Summary/Keyword: L-lactide

Search Result 187, Processing Time 0.024 seconds

Release Behavior of 5-FU from 5-FU/PLGA Wafer using Recrystallized PLGA and Monomer (재결정 PLGA와 단량체를 이용한 5-FU/PLGA 웨이퍼의 방출거동)

  • Park, Jung Soo;Choi, Myoung Kyu;Kim, Yun Tae;Lee, Jun Hee;Mo, Jong Hyun;Khang, Gilson;Rhee, John Moon;Shin, Hyung Shik;Lee, Hai Bang
    • Korean Chemical Engineering Research
    • /
    • v.46 no.2
    • /
    • pp.205-210
    • /
    • 2008
  • Poly(D,L-lactide-co-glycolide) (PLGA) has been widely used as carriers in controlled release delivery systems due to its biodegradability and relatively good biocompatibility. However, Release pattern of carriers fabricated using PLGA have disadvantage an initial burst within a few days, lag time several days and then sudden release changes. To solve these problems of PLGA, we fabricated PLGA wafer including monomer. Also, drug release behavior restraint sudden burst effect using recrystallization of PLGA. Recrystallized PLGA was characterized the morphological difference by SEM and in vitro release behavior measured by HPLC. The PLGA molecular weight analyzed to recognize monomer influence during degradation process of polymer using GPC. In this study, drug release duration cut short up to three days and was eliminated the lag time based on the bulk erosion.

Synthesis and Micellar Characterization of CBABC Type PLGA-PEO-PPO-PEO-PLGA Pentablock Copolymers

  • Seong, Haseob;Cho, Eun-Bum;Oh, Joongseok;Chang, Taihyun
    • Bulletin of the Korean Chemical Society
    • /
    • v.35 no.8
    • /
    • pp.2342-2348
    • /
    • 2014
  • Poly(lactic-co-glycolic acid) (PLGA) were grafted to both ends of Pluronic$^{(R)}$ F68 ($(EO)_{75}(PO)_{30}(EO)_{75}$) triblock copolymer to produce poly{(lactic acid)$_m$-co-(glycolic acid)$_n$}-b-poly(ethylene oxide)$_{75}$-b-poly(propylene oxide)$_{30}$-b-poly(ethylene oxide)$_{75}$-b-poly{(lactic acid)$_m$-co-(glycolic acid)$_n$} (PLGA-F68-PLGA) pentablock copolymers. Molecular weights of PLGA blocks were controlled and five kinds of pentablock copolymers with different PLGA block lengths were synthesized using in-situ ring-opening polymerization of D,L-lactide and glycolide with tin(II) 2-ethylhexanoate ($Sn(Oct)_2$) catalyst. PLGA-F68-PLGA pentablock copolymers were characterized by $^1H$- and $^{13}C$-NMR, GPC, and TGA. The numbers (2m, 2n) of repeating units for lactic acid and glycolic acid inside PLGA segments were obtained as (48, 17), (90, 23), (125, 40), (180, 59), and (246, 64), with $^1H$-NMR measurement. From NMR data, the resultant molecular weights were determined in the range of 12,700-29,700, which were similar to those obtained from GPC. Polydispersity index was increased in the range of 1.32-1.91 as the content of PLGA blocks increased. TG and DTG thermograms showed discrete degradation traces for PLGA and F68 blocks, which indicate the weight fractions of PLGA blocks in pentablock copolymers can be calculated by TG profile and it is possible to remove PLGA block selectively. Hydrodynamic radius and radius of gyration of pentablock copolymer micelle were obtained in the range of 46-68 nm and 31-49 nm, respectively, in very dilute (i.e. 0.005 wt %) aqueous solution of THF:$H_2O$ = 10:90 by volume at $25^{\circ}C$.

Effects of SIS/PLGA Porous Scaffolds and Muscle-Derived Stem Cell on the Formation of Tissue Engineered Bone (SIS/PLGA 담체와 근육유래 줄기세포를 이용한 생체조직공학적 골재생)

  • Kim Soon Hee;Yun Sun Jung;Jang Ji Wook;Kim Moon Suk;Khang Gilson;Lee Hai Bang
    • Polymer(Korea)
    • /
    • v.30 no.1
    • /
    • pp.14-21
    • /
    • 2006
  • Tissue engineering techniques require the use of a porous biodegradable/bioresorbable scaffold, which server as a three-dimensional template for initial cell attachment and subsequent tissue formation in both in vitro and in vivo. Small intestinal submucosa (SIS) has been investigated as a source of collagenous tissue with the potential to be used as biomaterials because of its inherent strength and biocompatibility. SIS-loaded poly(L-lactide-co-glicolide)(PLGA) scaffolds were prepared by solvent casting/particle leaching. Characterizations of SIS/PLGA scaffold were carried out by SEM, mercury porosimeter, and so on. Muscle-derived stem cells can be differentiated in culture into osteoblasts, chondrocytes, and even myoblasts by the controlling the culture environment. Cellular viability and proliferation were assayed by 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium-bromide(MTT) test. Osteogenic differential cells were analyzed by alkaline phosphatase(ALP) activity. SIS/PLGA scaffolds were implanted into the back of athymic nude mouse to observe the effect of SIS on the osteoinduction compared with controlled PLGA scaffolds. Thin sections were cut from paraffin embedded tissues and histological sections were conducted hematoxylin and eosin (H&E), Trichrome, and von Kossa. We observed that bone formatioin of SIS/PLGA hybrid scaffold as natural/synthetic scaffold was better thean that of only PLGA scaffold. It canb be explained that SIS contains various kinds of bioactive molecules for osteoinduction.

Local Drug Delivery System Using Biodegradable Polymers

  • Khang, Gil-Son;Rhee, John M.;Jeong, Je-Kyo;Lee, Jeong-Sik;Kim, Moon-Suk;Cho, Sun-Hang;Lee, Hai-Bang
    • Macromolecular Research
    • /
    • v.11 no.4
    • /
    • pp.207-223
    • /
    • 2003
  • For last five years, we are developing the novel local drug delivery devices using biodegradable polymers, especially polylactide (PLA) and poly(D,L-lactide-co-glycolide) (PLGA) due to its relatively good biocompatibility, easily controlled biodegradability, good processability and only FDA approved synthetic degradable polymers. The relationship between various kinds of drug [water soluble small molecule drugs: gentamicin sulfate (GS), fentanyl citrate (FC), BCNU, azidothymidine (AZT), pamidronate (ADP), $1,25(OH)_2$ vitamin $D_3$, water insoluble small molecule drugs: fentanyl, ipriflavone (IP) and nifedipine, and water soluble large peptide molecule drug: nerve growth factor (NGF), and Japanese encephalitis virus (JEV)], different types of geometrical devices [microspheres (MSs), microcapsule, nanoparticle, wafers, pellet, beads, multiple-layered beads, implants, fiber, scaffolds, and films], and pharmacological activity are proposed and discussed for the application of pharmaceutics and tissue engineering. Also, local drug delivery devices proposed in this work are introduced in view of preparation method, drug release behavior, biocompatibility, pharmacological effect, and animal studies. In conclusion, we can control the drug release profiles varying with the preparation, formulation and geometrical parameters. Moreover, any types of drug were successfully applicable to achieve linear sustained release from short period ($1{\sim}3$ days) to long period (over 2 months). It is very important to design a suitable formulation for the wanting period of bioactive molecules loaded in biodegradable polymers for the local delivery of drug. The drug release is affected by many factors such as hydrophilicity of drug, electric charge of drug, drug loading amount, polymer molecular weight, the monomer composition, the size of implants, the applied fabrication techniques, and so on. It is well known that the commercialization of new drug needs a lot of cost of money (average: over 10 million US dollar per one drug) and time (average: above 9 years) whereas the development of DDS and high effective generic drug might be need relatively low investment with a short time period. Also, one core technology of DDS can be applicable to many drugs for the market needs. From these reasons, the DDS research on potent generic drugs might be suitable for less risk and high return.

The Release of Albumin from PLGA and PCL Wafers Containing Natural and Synthetic Additives for Protein Delivery (단백질 전달체로서 천연 및 합성재료의 첨가에 따른 PLGA와 PCL웨이퍼로부터 알부민의 방출거동)

  • Hyun Hoon;Lee Jae Ho;Seo Kwang Su;Kim Moon Suk;Rhee Jhon M.;Lee Hai Bang;Khang Gilson
    • Polymer(Korea)
    • /
    • v.29 no.5
    • /
    • pp.468-474
    • /
    • 2005
  • PLGA and PCL copolymers initiated by carbitol as drug carriers were synthesized by ring-opening polymerization of L-lactide (LA), glycolide (GA), and $\varepsilon-caprolactone(\varepsilon-CL)$. Implantable wafers were simply fabricated by direct compression method after physical mixing of copolymers and bovine serum albumin-fluorescein isothiocyanate (BSA-FITC) as a model protein drug. The release amounts of BSA-FITC from wafers were determined by fluorescence intensity using the fluorescence spectrophotometer. Also, the release behavior of BSA-FITC on wafers was controlled by adding the additives such as collagen, small intestinal submucosa (SIS), poly(vinyl pyrrolidone) (PVP), and poly(thylene glycol) (PEG). The wafer prepared by PLGA and PCL exhibited slow release within $10\%$ for 30 days. But, those prepared by a variety of additives exhibited the controlled BSA release patterns with a dependence on the additive contents. furthermore, the wafers containing natural materials such as collagen and SIS showed more zero-order release profile than that with synthetic materials such as PVP and PEG. It was confirmed that the release of BSA from implantable wafers could be easily controlled by adding natural additives.

Miscibility of Melt-mixed PLLA/PMMA Blends for Optical Film Application (광학 필름 적용을 위한 용융혼합된 PLLA/PMMA 블렌드의 상용성 연구)

  • Park, Eun Ju;Kim, In Seok;Park, Sang Seok;Lee, Ho Sang;Lee, Moo Sung
    • Polymer(Korea)
    • /
    • v.37 no.6
    • /
    • pp.744-752
    • /
    • 2013
  • The miscibility between poly(L-lactide) (PLLA) and poly(methyl methacrylate) (PMMA) was investigated using thermal analyses for the purpose of developing birefringence-free material at oriented state. The effect of methyl acrylate (MA) units as comonomer of PMMA on the miscibility was also studied. All the blends prepared in this study show composition-dependent single $T_g$'s between those of blend components and high transparency over the visible region, indicating the miscibility at molecular level and no discernible effect of MA units on it. No phase separation was observed at elevated temperature of $280^{\circ}C$, higher than the degradation of PLLA and PMMA. The interaction energy density in PLLA/PMMA blends with 17 mol% of MA was measured to be $-0.74J/cm^3$ from the equilibrium melting temperature depression based on the Hoffman-Weeks method. The blends show zero-${\Delta}$n behavior at a specific mixing ratio and the drawing ratio of 3 due to compensation of intrinsic orientation birefringence. Birefringence dispersion of PLLA/PMMA5 blends was also measured to examine the possibility for quarter-wave plates or polarizer protective films.

A comparison of chlorhexidine release rate from three polymeric controlled release drug prototypes (제어방출형 소독제의 약물전달 체로 사용된 폴리머 유형에 따른 클로르헥시딘 제어 방출속도 비교)

  • Bok Young-Bin;Lee Doug-Youn;Lee Chang-Young;Kim Kyung-Nam;Kum Kee-Yeon
    • Restorative Dentistry and Endodontics
    • /
    • v.29 no.6
    • /
    • pp.548-552
    • /
    • 2004
  • Intracanal disinfection of infected root canal is one of important treatment procedure. This in vitro study aimed to evaluate whether the surface polymers of controlled release drug (CRD) can effectively control the release rate of chlorhexidine for root canal disinfection. Four CRD prototypes were prepared: Group A (n=12); The core device (absorbent paper point) was loaded with 40% CHX solution as control. Group B (n=12); same as group A, but the device was coated with chitosan. Group C (n=12); same as group A and then coated three times with 5% PMMA. Group D (n=12); same as group A and then coated three times with 3% PLGA. All CRD prototypes were soaked in 3 mL distilled water for experimental periods and the concentrations of released CHX from each CRD prototype were determined using a UV spectrophotometer. Results showed that release rate of CHX were the greatest in the non-coated group (control group), followed by the chitosan-coated group, the PLGA-coated group, and the PMMA-coated group (P < 0.05). This data indicate that surface polymers can control the release rate of CHX from the CRD prototypes.