• Title/Summary/Keyword: Entrapment Efficiency

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Production of Gemcitabine-Loaded Poly (L-lactic acid) Microparticles Using Supercritical Carbon Dioxide: Effect of Process Parameters (초임계 이산화탄소를 이용한 Gemcitabine 함유 PLLA 미립자 제조: 공정 변수의 영향)

  • Joo, Hyun-Jae;Jung, In-Il;Lim, Gio-Bin;Ryu, Jong-Hoon
    • KSBB Journal
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    • v.26 no.1
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    • pp.69-77
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    • 2011
  • In this study, poly (L-lactic acid) (PLLA) microparticles containing gemcitabine hydrochloride were prepared by a supercritical fluid process, called aerosol solvent extraction system (ASES), utilizing supercritical carbon dioxide as antisolvent. The influence of process parameters such as temperature, pressure, $CO_2$ and solution flow rate, solution concentration, and feed ratio of drug to polymer on the morphology and characteristics of the microparticles was studied in detail. The gemcitabine-loaded microparticles exhibited a spherical shape with a smooth surface. The entrapment efficiency of gemcitabine increased with increasing temperature, solution concentration and $CO_2$ flow rate and with decreasing drug/polymer feed ratio. The maximum drug loading obtained from the ASES process was found to be about 11%. The ASES-processed PLLA microparticles containing gemcitabine showed a relatively high initial burst due to the presence of surface pores on the microparticles and the poor affinity between drug and polymer.

Effect of Dextran Gel on Preparation of Nano-liposomes Loaded with Ginkgolide

  • Tong, Yuan;Chen, Yan;Pan, Jian;Huang, Li;Wang, Ruijun
    • Bulletin of the Korean Chemical Society
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    • v.31 no.9
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    • pp.2542-2546
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    • 2010
  • The objective of this paper was to investigate the effect of dextran gel on preparation of nano-liposomes loaded with ginkgolide. During preparation, Sephadex G75, G50 and G25 were added in the aqueous phase respectively. From the experiment, nano-liposomes prepared by dextran gels were found spherical and smooth. The result indicated that aperture of dextran gels were narrower, particle size of nano-liposomes was smaller (207.13 ~ 89.16 nm) and zeta potential was greater (-36.2 ~ -29.5 mV) in more negative. The study also revealed that differences of the entrapment efficiency and drug loading among the three types of nano-liposomes were not significant. In vitro drug release test demonstrated that nano-liposomes had a better controlled release. To conclude, by using dextran gel in the preparation of nano-liposome loaded with ginkgolide, the particle size could be effectively controlled and the drug stability could be improved.

Encapsulation of Lactic Acid in Starch by Extrusion for using as pH Regulated Binder of Meat Products

  • Hong, Geun-Pyo;Lee, Yeun-Sul;Baek, Ji-Yoo;Choi, Mi-Jung
    • Food Science of Animal Resources
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    • v.32 no.2
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    • pp.155-161
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    • 2012
  • This study was carried out to investigate the encapsulation of lactic acid in starch matrix for the application into emulsified sausages. For the encapsulation of lactic acid in starch, the extrusion method was applied, by the different extrusion pressure level. The particle size and morphology of lactic acid containing starch granules and the rate of release of lactic acid from those granules were determined by using Mastersizer$^{(R)}$, a scanning electron microscopy, and electrical conductivity. The size varied slightly depending upon the extruder pressure and influenced entrapment efficiency. Lactic acid was released more slowly, when the extruder had fewer holes, which meant higher extrusion pressure, than when the extruder had more holes. Extruder pressure is therefore critical for producing finer granules that can retain lactic acid longer, during the processing of meat products.

Transdermal Permeation of $[{^3}H]Acyclovir$ Using Niosome (니오솜을 이용한 $[^{3}H]$아시클로버의 경피투과)

  • Park, Sae-Hae;Lee, Soon-Young;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.28 no.1
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    • pp.43-50
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    • 1998
  • Niosomes are vesicles formed from synthetic non-ionic surfactants, offering an alternative to chemically unstable and expensive liposomes as a drug carrier. Non-ionic surfactant and cholesterol mixture film leads to the formation of vesicular system by hydration with sonication method. The formation of niosome was ascertained by negative staining of TEM. The entrapment efficiency of niosomal suspension was gradually increased with increasing the ratio of cholesterol to surfactant. It was found that the niosome with 6 : 4 (polyoxyethylene 2-cetyl ether: cholesterol) ratio was more stable than those with other ratios. The topical application of acyclovir(ACV) in the treatment of herpes simplex virus type 1(HSV-1) skin disease has a long history. There are an increasing number of reports, however, in which topical ACV therapy is not as effective as oral administration. Lack of efficacy with topical ACV has been hypothesized to reflect the inadequate delivery of drug to the skin. We investigated the permeation of niosome containing $[^{3}H]ACV$ in hairless mouse skin using Franz diffusion cell model. Permeation coefficient(P) of aqueous ACV was $6.7{\times}10^{-4}\;(cm/hr)$ and that of ACV in niosome was $23.4{\times}10^{-4}\;(cm/hr)$, suggesting about 3.5 times increase in the transdermal permeation.

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Antimicrobial Drug Release Scaffolds of Natural and Synthetic Biodegradable Polymers

  • Prabu, Periasamy;Kim, Kwan-Woo;Dharmaraj, Nallusamy;Park, Jong-Hoon;Khil, Myung-Seob;Kim, Hak-Yong
    • Macromolecular Research
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    • v.16 no.4
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    • pp.303-307
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    • 2008
  • A series of biodegradable polymeric scaffolds was prepared by using a combination of natural (collagen) and synthetic (poly(caprolactone)) (PCL) polymers in various compositions. These scaffolds were soft, spongy, porous and transparent in nature and were characterized by thermogravimetric analysis (TGA) and Fourier transform infrared (FT-IR) spectroscopy. The entrapment efficiency and drug release activity of the scaffolds were analyzed using penicillin and tetracycline as antimicrobial drugs. The drug release activity of the scaffolds with various combinations of collagen and PCL were studied by measuring the optical density in a spectrophotometer at the following time intervals: 1,4, 24, 48 and 60 h. These scaffolds showed better and continuous drug release for up to 60 h. Even after such a long duration, a portion of the drug remained entrapped in the scaffolds, indicating that they can be utilized for wound healing applications.

Preparation of Cyclosporin A-loaded Nanoparticles Containing Ethyl Myristate or Chitosan and Pharmacokinetics in Rats

  • Nam, Dae-Sik;;Lee, Woo-Kyoung
    • Journal of Pharmaceutical Investigation
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    • v.37 no.1
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    • pp.15-22
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    • 2007
  • An oil-in-water solvent evaporation method was used to prepare the cyclosporin A (CyA)-loaded nanoparticles varying in poly (D,L-lactide-co-glycolide) (PLGA) polymer (RG 502H, RG 503H) and the amount of additive ethyl myristate (EM) or chitosan (CS). The particles were characterized for drug loading and entrapment efficiency by HPLC, surface morphology by scanning electron microscopy, particle size by dynamic light scattering and surface charge by Zetapotential. The results showed drug loadings ranging from 10.9% to 15.8% with high encapsulation efficiency (82.0-97.8%). SEM and DLS studies showed discrete and spherical particles with smooth surfaces and mean size ranging 257.6-721.7 nm. The additive EM or CS did not change the mean sizes of the nanoparticles, whereas by the coating effect of CS, the Zetapotential values of the CS-added nanoparticles were moved to the more positive direction as the amount of CS was increased. From the pharmacokinetic analysis, the nanoparticles formulations showed the higher bioavailability and MRT than $Neoral^{\circledR}$ While little adding effect of EM or CS was detected in pharmacokinetic profile when RG 503H was used as polymer carrier, more noticeable different pharmacokinetic behaviors could be observed in case of RC 502H. EM incorporation was found to elevate the $K_{el}$, whereas CS coating resulted in the decrease of F and $K_{el}$, which seems to be due to the function of CS as a barrier and a mucoadhesive coating.

Properties of β-carotene-loaded chitosan/hyaluronic acid nanocapsules: solubility and redispersibility (베타카로틴 함유 키토산/하이알루론산 나노캡슐의 용해도 및 재분산성 특성)

  • An, Eun Jung;Lee, Ji-Soo;Lee, Hyeon Gyu
    • Korean Journal of Food Science and Technology
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    • v.54 no.1
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    • pp.66-74
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    • 2022
  • To improve the solubility of β-carotene, three types of β-carotene-loaded nanocapsules were prepared using chitosan (CS) and two cross-linkers, sodium tripolyphosphate (TPP) and hyaluronic acid (HA), alone or in combination (CS-TPP, CS-TPP-HA, and CS-HA). The entrapment efficiency of all nanocapsules significantly increased with an increase in TPP and HA, with the efficiency ranging from 95% to 99%. The solubility of β-carotene was significantly improved by CS nanoencapsulation before and after lyophilization and during storage. CS/HA nanoencapsulation significantly improved (by 11-fold) the water solubility of β-carotene. In particular, CS/HA nanoencapsulation was the most effective in terms of not only the solubility of β-carotene, but also the redispersibility ratio. Therefore, CS/HA encapsulation could be useful for improving the solubility of poorly soluble active ingredients, such as β-carotene.

Studies on Microbial Penicillin Amidase (II) Characteristics and the Reactor Performance of Whole Cell Immobilized Penicillin Amidase of Escherichia coli (미생물 페니실린 아미다제에 관한 연구 (II) E. coli의 균체 고정화 페니실린 아미다제의 특성 및 반응조에 관한 연구)

  • Seong, Baik-Lin;Kim, Bong-Hee;Mheen, Tae-Iek;Moon H. Han
    • Microbiology and Biotechnology Letters
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    • v.9 no.1
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    • pp.35-44
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    • 1981
  • Whole cell penicillin amidase of Escherichia coli was immobilized by entrapment in gelatin followed by extrusion and crosslinking with glutaraldehyde. The immobilized engyme preparation demonstrated the recovery yield of activity up to 70% and good stability during storage and operation. The half life of activity decay during the operation was estimated to be about 50 days. The optimum pH and temperature for both of immobilized and soluble enzyme are 8.5 and 5$0^{\circ}C$, respectively. No significant change was demonstrated in the effect of pH and temperature, but the increase in heat stability at high temperature was observed in the case of the immobilized enzyme. It was found that the plug flow reactor could be operated favorably since the pH drop along the column path due to tile reaction product was minimized by employing substrate solution with moderate buffer strength. The optimal condition of reactor operation was discussed with regard to the effect of substrate concentration and the residence time on the conversion efficiency and productivity.

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Sustained Release Injectable of Recombinant Bovine Somatotropin in Biodegradable Poly(D,L-lactide-co-glyceride) Microspheres (생분해성 폴리락티드/글리콜리드 미립구를 이용한 재조합 소 성장호르몬(rBST)의 지속성주사제 설계)

  • Jeon, Hong-Ryeol;Lee, Bong-Sang;Kown, Do-W;Yoon, Mi-Kyoung;Jeon, Hyun-Joo;Shin, Taek-Hwan;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.32 no.3
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    • pp.199-207
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    • 2002
  • In order to develop a sustained release formulation of bovine somatotropin (BST), which has been used to increase the body weight of oxen or the milk production of dairy cows, poly(D,L-lactide-co-glyceride)(PLGA) microspheres were made by W/O/W multiple emulsification method and solvent extraction method. Physical properties including particle size, drug entrapment, drug release, protein denaturation, and in vivo body weight increase in rats were characterized. The size of the microspheres was increased as the molecular weight of PLGA increased. When Span 65 and stearic acid during preparation were added, the size was decreased but the amount of surface protein was increased, resulting in a high loading efficiency, with fast release of BST from the microspheres. Aggregation or fragmentation of BST by SDS-PAGE during microsphere preparation and drug release study was not observed. Body weight of Sprague-Dawley's male rats was significantly increased after subcutaneous administrations of BST-loaded PLGA microspheres. There was a good correlation between in vivo weight gain and in vitro release rate of microspheres. PLGA microspheres with a high surface protein ratio could be a good candidate for the sustained delivery of BST.

Preparation and Drug Release of All-Trans Retinoic Acid-Loaded Poly(L-lactic acid) Nanoparticles (레티노산 함유 폴리락탄산 나노입자의 제조 및 약물 방출)

  • Chae, Ji-Man;Lee, Kyung-Man;Kim, In-Sook;Lee, Yong-Bok;Shin, Sang-Chul;Oh, In-Joon
    • Journal of Pharmaceutical Investigation
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    • v.34 no.5
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    • pp.401-406
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    • 2004
  • To develop an intravenous delivery system of all-trans retinoic acid (ATRA) for the cancer therapy, poly(L-lactic acid) nanoparticles were prepared and characterized. Emulsification-solvent evaporation method was chosen to prepare submicron sized nanoparticles. Spherical nanoparticles less than 200 nm in diameter with narrow size distribution were prepared, and the entrapment efficiency of drug was more than 95%. The endothermic peak at $183^{\circ}C$ and X-ray crystallographic peak of ATRA appeared in the nanoparticle system, suggesting the inhibition of crystallization of ATRA by polymer adsorption during the precipitation process. ATRA was released at $37^{\circ}C$ for 60 days and the release rate was dependent on the concentration of drug incorporated in the nanoparticles. While ATRA was unstable in the light, it was very stable at $4^{\circ}C$. These results suggest the usefulness of PLA nanoparticles as a sustained and prolonged release carrier for ATRA.