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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
> Journal Vol & Issue
Journal of Pharmaceutical Investigation
Journal Basic Information
Journal DOI :
The Korean Society of Pharmaceutical Sciences and Technology
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Volume & Issues
Volume 40, Issue 6 - Dec 2010
Volume 40, Issue 5 - Oct 2010
Volume 40, Issue 4 - Aug 2010
Volume 40, Issue 3 - Jun 2010
Volume 40, Issue spc - May 2010
Volume 40, Issue 2 - Apr 2010
Volume 40, Issue 1 - Feb 2010
Selecting the target year
Self-organized Nanogels of Polysaccharide Derivatives in Anti-Cancer Drug Delivery
Park, Sin-Jung ; Na, Kun ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 201~212
DOI : 10.4333/KPS.2010.40.4.201
Self-organized nanogels from polysaccharide derivatives offer a promising approach in treatment of cancer due to their flexibility in chemistry and their ability to improve the therapeutic index of a drug by modifying biodistribution by their preferential localization at target sites and lower distribution in normal healthy tissues. These properties have promoted studies of active cancer targeting by self-organized nanogels for even better accumulation in solid tumors. However although many researchers have reported their potential by using cell culture systems and small animal tumor models in cancer therapy, these nanogels need more decoration such as conjugation with targeting moiety and endowment of stimuli-sensitivity for precise targeting of the cancer site. In this review, we summarize the recent efforts in developing novel targeting approaches via active endocytosis and stimuli-sensitive systems responding to hyperthermic or acidic tumor pH conditions.
Structural Analysis of 5-aminosalicyl-L-glutamic Acid, a Colon-specific Prodrug of 5-aminosalicylic Acid, for Colon-specific Deconjugation
Kim, Ji-Hye ; Kim, Jung-Yoon ; Lee, Yong-Hyun ; Kim, Young-Mi ; Jung, Yun-Jin ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 213~218
DOI : 10.4333/KPS.2010.40.4.213
In a previous paper, we showed that 5-aminosalicyl-L-aspartic acid (5-ASA-Asp) has much greater deconjugation efficiency in the cecal contents than does 5-aminosalicyl-L-glutamic acid (5-ASA-Glu). To explore a reason for ineffective deconjugation of 5-ASA-Glu, structural analysis of the conjugate was performed. Aromatic acyl-L-glutamic acid derivatives, N-benzoyl-glumatic acid (BA-Glu), N-(2-hydroxybenzoyl)-glutamic acid (SA-Glu), N-(3-aminobenzoyl)-glutamic acid (3-ABA-Glu) and N-(4-aminobenzoyl)-glutamic acid (4-ABA-Glu), were prepared and incubated in the cecal contents. The deconjugation rates were compared with that of 5-ASA-Glu. The order of the rates was BA-Glu
5-ASA-Glu. The deconjugation of the aromatic acyl-L-glutamic acid derivatives was carried out by enzyme(s) in the cecal contents since the deconjugation did not occur in the autoclaved cecal contents and on incubation with N-benzoyl-D-glutamic acid. Our data suggest that the 2-hydroxyl group in 5-ASA is ascribed to the poor deconjugation of 5-ASA-Glu in the cecal contents.
Synthesis and Characterization of Hyaluronic Acid-α-Cyclodextrin Conjugate as the Potential Carrier of PEGylated Drugs
Sivasubramanian, Maharajan ; Park, Jae-Hyung ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 219~223
DOI : 10.4333/KPS.2010.40.4.219
The hyaluronic acid (HA) conjugate bearing
-CD) was synthesized as the potential carrier of poly(ethylene glycol) (PEG)-drug conjugates. The HA conjugate was prepared by the reaction between the carboxylic acid of HA and the primary amine of
-CD in the presence of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide and 1-hydroxybenzotriazole. The chemical structure of the conjugate was confirmed using
NMR and FT-IR spectroscopy. The conjugate could form nano-sized particles in the presence of PEG by forming the inclusion complexes between
-CD at the backbone of HA, which was demonstrated using electrophoretic light scattering and field emission transmission electron microscopy. It is anticipated that this novel kind of nanoparticles can serve as a useful delivery system for PEGylated drugs.
Meta-analysis of Inline Filtration Effects on Post-infusion Phlebitis Caused by Particulate Contamination of Intravenous Administration
Ku, Hye-Min ; Kim, Ji-Yeon ; Kang, Suk-Hyun ; Lee, Eui-Kyung ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 225~230
DOI : 10.4333/KPS.2010.40.4.225
The particulate contamination of intravenously administered fluid has been of major concern. One of the most common complications associated with long term i.v. therapy is post-infusion phlebitis (PIP). We undertook a systematic review and meta-analysis of the effect of inline filters on PIP. An electronic search of Medline, KoreaMed, and KRIST was conducted to identify randomized controlled trials evaluating the effect of inline filters. Meta-analysis was undertaken using STATA 10. A total of 62 literatures were retrieved, of which 7 were included in meta-analysis. Inline filtration for intravenous infusion significantly reduced by 39% of the incidence of phlebitis, with a relative risk of 0.61 (95% CI 0.41-0.90, p=0.012). Therefore, inline filtration is a highly effective means of decreasing the incidence of infusion phlebitis and should be considered as a part of intravenous therapy.
Sustained Release of Anthocyanin from Porous Poly(lactic-co-glycolide) Microsparticles Developed for the Treatment of Chronic Obstructive Pulmonary Disease
Yoo, Na-Young ; Baik, Hye-Jung ; Lee, Bo-Reum ; Youn, Yu-Seok ; Oh, Kyung-Taek ; Lee, Eun-Seong ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 231~236
DOI : 10.4333/KPS.2010.40.4.231
This study was to fabricate the porous poly(lactide-co-glycolide) (PLGA) microparticles with anthocyanin (as a model antioxidant) for pulmonary drug delivery. The highly porous PLGA microparticles were prepared by the waterin-oil-in-water (
) multi-emulsion method, followed by the decomposition of ammonium bicarbonate (AB) in
phase to the base of ammonia, carbon dioxide and water vapor at
, making a porous structure in PLGA microparticles. Herein, hyaluronate (HA), a viscous polysaccharide, was incorporated in the porous microparticles for sustained anthocyanin release. In in vitro release studies, the anthocyanin release from the porous microparticles with HA continued up to 24 hours, while the porous microparticles without HA released 80 wt.% of encapsulated anthocyanin within 2 hours. In addition, these microparticle are expected to be effectively deposited at a lung epithelium due to its high porosity (low density) and avoid alveolar macrophage's uptake in the lung due to its large particle size. We believe that this system has a great pharmaceutical potential as a long acting antioxidant for relieving the oxidative stress in chronic obstructive pulmonary disease (COPD).
Material Properties and Compressibility Using Heckel and Kawakita Equation with Commonly Used Pharmaceutical Excipients
Choi, Du-Hyung ; Kim, Nam-Ah ; Chu, Kyung-Rok ; Jung, Youn-Jung ; Yoon, Jeong-Hyun ; Jeong, Seong-Hoon ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 237~244
DOI : 10.4333/KPS.2010.40.4.237
This study investigated basic material properties and compressibility of commonly used pharmaceutical excipients. Five classes of excipients are selected including starch, lactose, calcium phosphate, microcrystalline cellulose (MCC), and povidone. The compressibility was evaluated using compression parameters derived from Heckel and Kawakita equation. The Heckel plot for lactose and dicalcium phosphate showed almost linear relationship. However, for MCC and povidone, curves in the initial phase of compression were observed followed by linear regions. The initial curve was considered as particle rearrangement and fragmentation and then plastic deformation at the later stages of the compression cycle. The Kawakita equation showed MCC exhibited higher compressibility, followed by povidone, lactose, and calcium phosphate. MCC undergoes significant plastic deformation during compression bringing an extremely large surface area into close contact and facilitating hydrogen bond formation between the plastically deformed, adjacent cellulose particles. Lactose compacts are consolidated by both plastic deformation and fragmentation, but to a larger extent by fragmentation. Calcium phosphate has poor binding properties because of its brittle nature. When formulating tablets, selection of suitable pharmaceutical excipients is very important and they need to have good compression properties with decent powder flowability. Material properties tested in this study might give a good guide how to select excipients for tablet formulations and help the formulation scientists design the optimum ones.
Pharmaceutical Potential of Gelatin as a pH-responsive Porogen for Manufacturing Porous Poly(d,l-lactic-co-glycolic acid) Microspheres
Kim, Hyun-Uk ; Park, Hong-Il ; Lee, Ju-Ho ; Lee, Eun-Seong ; Oh, Kyung-Taek ; Yoon, Jeong-Hyun ; Park, Eun-Seok ; Lee, Kang-Choon ; Youn, Yu-Seok ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 245~250
DOI : 10.4333/KPS.2010.40.4.245
Porous poly(lactic-co-glycolic acid) microspheres (PLGA MS) have been utilized as an inhalation delivery system and a matrix scaffold system for tissue engineering. Here, gelatin (type A) is introduced as an extractable pH-responsive porogen, which is capable of controlling the porosity and pore size of PLGA microspheres. Porous PLGA microspheres were prepared by a water-in-oil-in-water (
) double emulsification/solvent evaporation method. The surface morphology of these microspheres was examined by varying pH (2.0~11.0) of water phases, using scanning electron microscopy (SEM). Also, their porosity and pore size were monitored by altering acidification time (1~5 h) using a phosphoric acid solution. Results showed that the pore-forming capability of gelatin was optimized at pH 5.0, and that the surface pore-formation was not significantly observed at pHs of < 4.0 or > 8.0. This was attributable to the balance between gel-formation by electrostatic repulsion and dissolution of gelatin. The appropriate time-selection between PLGA hardening and gelatin-washing out was considered as a second significant factor to control the porosity. Delaying the acidification time to ~5 h after emulsification was clearly effective to make pores in the microspheres. This finding suggests that the porosity and pore size of porous microspheres using gelatin can be significantly controlled depending on water phase pH and gelatin-removal time. The results obtained in this study would provide valuable pharmaceutical information to prepare porous PLGA MS, which is required to control the porosity.
Effect of pH on the Formation of Acylated Octreotides by Poly(lactide-co-glycolide)
Na, Dong-Hee ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 251~254
DOI : 10.4333/KPS.2010.40.4.251
The formation of acylated peptide impurities in poly(lactide-co-glycolide) (PLGA) formulations is one of the major challenges to the development of successful sustained-release product. Octreotide, synthetic analogue of somatostatin, has been identified to be acylated in PLGA microsphere formulations. The purpose of this study was to investigate the pH effect on the formation of acylated octreotides by PLGA. In the incubation with PLGA in 0.1 M phosphate buffer at pH 7.4, approximately 98% of octreotide adsorbed to PLGA through 14 days and 66.3% of acylated octreotides were produced after 42 days, whereas the interaction of octreotide with PLGA was significantly inhibited in the incubation at pH 4, in which the acylated octreotides were observed to be 9.2% after 42 days. In the interaction study at pH 4.1-7.4, the production of acylated octreotides was demonstrated to be dependent on environmental pH. Below pH 5.0, the acylation of octreotide was significantly inhibited. This study indicates that the pH is the major factor for the formation of acylated octreotide in PLGA formulations.
Physiochemical Properties of Binary Pluronic Systems for Reversal of Multi-drug Resistant (MDR) Cancers
Yun, Jung-Min ; Park, Ga-Young ; Kim, Ha-Hyung ; Lee, Jae-Hwi ; Lee, Eun-Seong ; Youn, Yu-Seok ; Lee, Beom-Jin ; Oh, Young-Taik ; Oh, Kyung-Taek ;
Journal of Pharmaceutical Investigation, volume 40, issue 4, 2010, Pages 255~261
DOI : 10.4333/KPS.2010.40.4.255
Pluronic as pharmaceutical excipients are listed in the US and British Pharmacopoeia. In particular, Pluronics exist as different compositions and display abundant phases as self-assembling into polymeric micelles with various morphologies depending on the aqueous solvent quality, the composition of structure, and hydrophilic-lipophilic balance (HLB). Pluronics were also known as a P-gp modulator, which was exploited as a reversal molecule of multi-drug resistant (MDR) cancers. We selected a lamella forming Pluronic L92 which has high hydrophobicity and relatively long PEO block among L series of Pluronics. The dispersion of L92 showed great size particles and low stability. To increase the stability and to decrease the particle size, secondary Pluronics (F68, F88, F98, F127, P85, P105, and P123) with relatively long PEO chain were added into 0.1 wt% Pluronic L92 dispersion. The stability of binary systems was increased due to incorporated long PEO chain. Their particle sizes slightly decreased to over 200~400 nm and their solubilization capacity of binary systems didn't change except Pluronic L92/P123 mixtures. The L92/P123 systems showed ca. 100 nm sizes and lowest turbidity among the all systems. The solubilization capacity of 0.1 wt% L92/0.1 wt% P123 was slightly increased compared to 0.1 wt% L92 mono system and other binary systems. These nano-sized binary systems may have potential as alternative drug delivery systems with simple preparation method and overcome the drawbacks of mono systems such as low stability and loading capacity.