• Title, Summary, Keyword: drug encapsulation efficiency

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Control of Encapsulation Efficiency and Initial Burst in Polymeric Microparticle Systems

  • Yeo, Yeon;Park, Ki-Nam
    • Archives of Pharmacal Research
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    • v.27 no.1
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    • pp.1-12
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    • 2004
  • Initial burst is one of the major challenges in protein-encapsulated microparticle systems. Since protein release during the initial stage depends mostly on the diffusional escape of the protein, major approaches to prevent the initial burst have focused on efficient encapsulation of the protein within the microparticles. For this reason, control of encapsulation efficiency and the extent of initial burst are based on common formulation parameters. The present article provides a literature review of the formulation parameters that are known to influence the two properties in the emulsion-solvent evaporation/extraction method. Physical and chemical properties of encapsulating polymers, solvent systems, polymer-drug interactions, and properties of the continuous phase are some of the influential variables. Most parameters affect encapsulation efficiency and initial burst by modifying solidification rate of the dispersed phase. In order to prevent many unfavorable events such as pore formation, drug loss, and drug migration that occur while the dispersed phase is in the semi-solid state, it is important to understand and optimize these variables.

Stability and drug release properties of liposomes containing cytarabine as a drug carrier

  • Kim, Chong-Kook;Park, Dong-Kyu
    • Archives of Pharmacal Research
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    • v.10 no.2
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    • pp.75-79
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    • 1987
  • Liposomes were studied as a drug delivery system. Multilamellar vesicles, small unilamellar vesicles and large unilamellar vesicles containing cytarabine were prepared using egg yolk lecithin and cholesterol. Large unilamellar vesicles showed the highest encapsulation efficiency of all and their encapsulation efficiency increased as the buffer volume decreased. Cholesterol increased the stability of liposomal drug products as drug carriers and reduced the permeability of drug across the liposomal membrane. The release rate of cytarabine increased with incubation temperature and decreased with cholesterol incorporation in liposomal membrane. The release mechanism of cytarabine from large unilamellar vesicles in vitro was chiefly due to simple diffusion across the liposomal membrane rather than liposomal rupture.

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Preparation of Eudragit coated solid lipid nanoparticles (SLN) for hydrophilic drug delivery

  • Han, Sung-Chul;Yoon, Hee-Sun;Lee, Ki-Young;Kim, Yeon-Zu;Kim, Dong-Woon
    • 한국생물공학회:학술대회논문집
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    • pp.655-659
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    • 2003
  • Solid lipid nanoparticle (SLN) system has been attracted increasing attention during last few years as a potential drug delivery carrier However, the SLN have disadvantage of low encapsulation efficiency for hydrophilic drug. In this study, for increase it's encapsulation efficiency, we prepared the $Eudragit^{\circledR}$ L100-55 (eudragit) coated SLN(E-SLN) based on solvent evaporation method and melt dispersion technique, and analyzed their physicochemical properties in terms of particle size, morphology, and encapsulation efficiency. As a result, they have a ${\pm}150$ nm particle size, spherical shape, and $10^{\sim}25$ % loading efficiency. SLN consists of coconut oil as core material, ascorbic acid and okyong-san as hydrophilic drug.

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Effect of Bovine Serum Albumin on the Stability of Methotrexate-encapsulated Liposomes

  • Kim, Chong-Kook;Kim, Han-Sung;Lee, Beum-Jin;Han, Jeong-Hee
    • Archives of Pharmacal Research
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    • v.14 no.4
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    • pp.336-341
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    • 1991
  • The effect of bovine serum albumin (BSA) on the encapsulation efficiency and stability of liposomes containing methotrexate (MTX) having different surface charges and cholesterol contents were investigated. The encapsulation efficiency of MTX was lower and the release of MTX was faster by the addition of BSA. The leaking of MTX from lipid bilayer depends upon the BSA concentrations. These results may be derived from the interaction of BSA with lipid bilayers. The dynamic structural changes of BSA were monitored indirectly using circular dichroism spectra. Observed dynamic structural changes of BSA with liposomes are presumed to reflect the interaction of BSA with liposomes. Negatively charged liposomes have more strong interaction with BSA than neutral and positively charged liposomes. BSA attacks lipid bilayers whether it is at the inner or at the outer phase of lipid bilayer and induces leakage of entrapped MTX. Especially, negatively charged liposomes are more sensitive than others. The inclusion of cholesterol in the lipid layers inhibits the interaction of BSA with liposomes and shows protective effect against BSA-induced leakage of MTX. To endure the attacking of BSA liposomes as drug carriers should be made using cholesterol.

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Development of SS-AG20-loaded Polymeric Microparticles by Oil-in-Water (o/w) Emulsion Solvent Evaporation and Spray Drying Methods for Sustained Drug Delivery

  • Choi, Eun-Jung;Bai, Cheng-Zhe;Hong, A-Reum;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • v.33 no.10
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    • pp.3208-3212
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    • 2012
  • Controlled drug delivery systems employing microparticles offer lots of advantages over conventional drug dosage formulations. Microencapsulation technique have been conducted with biodegradable polymers such as poly(lactic-co-glycolic acid) (PLGA) and poly(lactic acid) (PLA) for its adjustable biodegradability and biocompatibility. In this study, we evaluated two techniques, oil-in-water (o/w) emulsion solvent evaporation and spray drying, for preparation of polymeric microparticles encapsulating a newly synthesized drug, SS-AG20, for the long-term drug delivery of this low-molecular-weight drug with a very short half-life. Drug-loaded microparticles prepared by the solvent evaporation method showed a smoother morphology; however, relatively poor encapsulation efficiency and drastic initial burst were discovered as drawbacks. Spray-dried drug-loaded microparticles had an imperfect surface with pores and distorted portions so that its initial burst was critical (70.05-87.16%) when the preparation was carried out with a 5% polymeric solution. By increasing the concentration of the polymer, the morphology was refined and undesirable initial burst was circumvented (burst was reduced to 35.93-74.85%) while retaining high encapsulation efficiency. Moreover, by encapsulating the drug with various biodegradable polymers using the spray drying method, gradual and sustained drug release, for up to 2 weeks, was achieved.

Preparation and Evaluation of Chrysin Encapsulated in PLGA-PEG Nanoparticles in the T47-D Breast Cancer Cell Line

  • Mohammadinejad, Sina;Akbarzadeh, Abolfazl;Rahmati-Yamchi, Mohammad;Hatam, Saeid;Kachalaki, Saeed;Zohreh, Sanaat;Zarghami, Nosratollah
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.9
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    • pp.3753-3758
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    • 2015
  • Background: Polymeric nanoparticles are attractive materials that have been widely used in medicine for drug delivery, with therapeutic applications. In our study, polymeric nanoparticles and the anticancer drug, chrysin, were encapsulated into poly (D, L-lactic-co-glycolic acid) poly (ethylene glycol) (PLGA-PEG) nanoparticles for local treatment. Materials and Methods: PLGA: PEG triblock copolymers were synthesized by ring-opening polymerization of D, L-lactide and glycolide as an initiator. The bulk properties of these copolymers were characterized using 1H nuclear magnetic resonance spectroscopy and Fourier transform infrared spectroscopy. In addition, the resulting particles were characterized by scanning electron microscopy. Results: The chrysin encapsulation efficiency achieved for polymeric nanoparticles was 70% control of release kinetics. The cytotoxicity of different concentration of pure chrysin and chrysin loaded in PLGA-PEG ($5-640{\mu}M$) on T47-D breast cancer cell line was analyzed by MTT-assay. Conclusions: There is potential for use of these nanoparticles for biomedical applications. Future work should include in vivo investigation of the targeting capability and effectiveness of these nanoparticles in the treatment of breast cancer.

Preparation and Evaluation of Temperature Sensitive Liposomes Containing Adriamycin and Cytarabine

  • Kim, Chong-Kook;Lee, Suk-Kyeong;Lee, Beom-Jin
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.129-133
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    • 1993
  • Temperature sensitive liposomes(TSL) containing adriamycin (ADM) and cytarabine (Ara-C) were prepared. ADM and Ara-C were selected as model compounds of amphiphilic and hydrophilic drug, respectively. Encapsulation efficiency of ADM entrapped into TSL was about twice greater than that of Ara-C. It might be due to different polarity of the drug, Lipid compositions of TSL had no effect on the encapsulation efficiency of drugs. Thermal behavior of TSL using a differential scanning calorimetry (DSC) was also investigated. Phase transition of TSL using a differential scanning calorimetry (DSC) was also investigated. Phase transition temperature $(T_c)$ of TSL was dependent on the lipid compositions of TSL ADM broadened thermogram of TSL but Ara-C did not. However, $T_c$ of TSL was not changed by any drug. Release rate of drugs was highly dependent on temperature. The release profile of ADM was similar to that of Ara-C. The maximum release rate of drugs from TSL was occurred at the near $T_c$ and observed at $39-41^\circ{C}$ for DPPC (Dipalmitoylphosphatidylcholine) only, $52-54^\circ{C}$ for DPPC and DSPC (1:1), respectively. Effect of human serum alburmin (HAA) on the release rate of ADM was investigated. HSA had no significant effect on the release of ADM below $T_c$. However, ADM release from TSL was increased at the near and above $T_c$. The HSA-induced leakage of drug may result from the interaction of liposomal constituents with HSA structure at the near TEX>$4^\circ{C}$. From the fact that the release profiles of ADM from freshly prepared TSL and stored TSL for 1 week at TEX>$4^\circ{C}$ was not changed, the TSL was considered to be stable for at least 1 week at TEX>$4^\circ{C}$. Based on these findings, TSL may be useful to deliver drugs to preheated target sites due to its thermal behaviors.

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Preparation and Characterization of Bovine Serum Albumin-loaded Cationic Liposomes: Effect of Hydration Phase

  • Park, Se-Jin;Jeong, Ui-Hyeon;Lee, Ji-Woo;Park, Jeong-Sook
    • Journal of Pharmaceutical Investigation
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    • v.40 no.6
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    • pp.353-356
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    • 2010
  • Although liposomes have been applied as drug delivery systems in various fields, the usage was limited due to the low encapsulation efficiency compared to other carrier systems. Here, cationic liposomes were prepared by mixing 1,2-dioleoyl-3-trimethylammoniopropane (DOTAP) as a cationic lipid, 1,2-dioleoyl-sn-glycerol-phosphoethanolamine (DOPE) and cholesterol (CH), and the liposomes were hydrated by varying the aqueous phases such as phosphate-buffered saline (PBS), 5% dextrose, and 10% sucrose in order to improve the encapsulation efficiency of bovine serum albumin (BSA). The particle size and zeta potential were determined by dynamic light scattering method and in vitro release patterns were investigated by spectrophotometry. Particle size and zeta potential of liposomes were varied depending on the ratio of DOTAP/DOPE/CH in range of 270-350 nm and 0.8-9.7 mV, respectively. Moreover, the addition of polyethylene glycol (PEG) improved the encapsulation efficiency from 37% to 43% as well as reduced particle sizes of liposomes while the liposomes were hydrated in PBS. When the liposomes were hydrated with 10% sucrose, the encapsulation efficiency of BSA was higher than any other groups. Whereas PBS was used as hydration solution, lower encapsulation efficiency was obtained compared with other groups. More than 60% of BSA was released from the liposomes hydrated with 10% sucrose; thereafter another 20% of BSA was released. Therefore, release pattern of BSA from cationic liposomes was extended release in this study. From the results, cationic liposomes dispersed in 10% sucrose would be potential carrier with high encapsulation efficiency.

Preparation of Solid Dosage Form containing SMEDDS of Simvastatin by Microencapsulation (심바스타틴 자가유화약물전달시스템의 마이크로캡슐화를 통한 고형제제의 개발)

  • Kang, Bok-Ki;Yoon, Bok-Young;Seo, Kwang-Su;Jeung, Sang-Young;Kil, Hee-Joo;Khang, Gil-Son;Lee, Hai-Bang;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.33 no.2
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    • pp.121-127
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    • 2003
  • The objective of this study was to solidify the simvastatin self-microemulsifying drug delivery system (SMEDDS) and to improve the encapsulation efficiency of solidified alginate beads using sodium alginate. Typical simvastatin SMEDDS was composed of various oils, surfactants and cosurfactants. Also solidified-alginate beads was prepared by crosslinking liquid emulsion mixtures containing sodium alginate and other excipients (cetylpyridinum chloride (CP-Cl), hydroxypropyl methylcellulose, starch and so on). in $CaCl_2$ solution, it has been investigated that the drug release pattern and encapsulation efficiency were varied with the ratio of cationic lipid (CP-Cl). Solidified sodium alginate beads containing simvastatin SMEDDS were redispersed into media without re-aggregation. Oil droplet size of redispersed solidified-beads in media produced smaller than the initial size. The density of beads and drug loading amount were increased with increasing cationic lipid content. These systems have advantages of storage stability and predictability of drug release rate.

Preparation of Gemcitabine-Loaded Methoxy Poly(ethylene glycol)-b-Poly(L-lactide) Microparticles Using W/O/W Double Emulsion (W/O/W 다중유화법을 이용한 젬시타빈 함유 Methoxy Poly(ethylene glycol)-b-Poly(L-lactide) 미립자 제조)

  • Ryu, Jong-Hoon;Jung, In-Il;Lee, Ji-Eun;Lim, Gio-Bin
    • KSBB Journal
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    • v.26 no.4
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    • pp.333-340
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    • 2011
  • In this study, gemcitabine-loaded methoxy poly(ethylene glycol)-b-poly(L-lactide) (MPEG-PLLA) microparticles with different PEG block lengths were prepared by a W/O/W double emulsion technique. The present study focuses on the investigation of the influence of various preparative parameters such as the ratio of internal water phase and oil phase, polymer concentration, solvent composition of organic phase and salt concentration of external water phase on the morphology and encapsulation efficiency of the microparticles. The microparticles fabricated at high volume ratios of internal water phase to oil phase and at high polymer concentrations showed a relatively high encapsulation efficiency and low porosity. When a dichloromethane/ethyl acetate mixture was used as solvent, both the encapsulation efficiency and drug loading of the microparticles decreased as the level of ethyl acetate increased. The addition of a salt (NaCl) to the external water phase significantly improved the encapsulation efficiency up to 40%, and the microparticles became more spherical with their size and porosity decreased.