• Title/Summary/Keyword: drug-release

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Particle Size Distribution, Drug Loading Capacity and Release Profiles of Solid Lipid Nanoparticles of Phenylpropionic Acids (페닐프로피온산계 해열진통제 고형지질나노입자의 입도분포와 약물봉입 및 용출특성)

  • Kim, Yoon-Sun;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.28 no.4
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    • pp.249-255
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    • 1998
  • Solid Lipid Nanoparticle(SLN), one of the colloidal carrier systems, has many advantages such as good biocompatibility, low toxicity and stability. In this paper, the effects of drug lipophilicity and surfactant on the drug loading capacity, particle size and drug release profile were examined. SLNs were prepared by homogenization of melted lipid dispersed in an aqueous surfactant solution. Ketoprofen, ibuprofen and pranoprofen were used as model drugs and tweens and poloxamers were tested for the effect of surfactant. Mean particle size of prepared SLNs was ranged from 100 to 150nm. The drug loading capacity was improved with the most lipophilic drug and low concentration of surfactant. Particle size and polydispersity of SLNs were changed according to the used lipid and surfactant. The rates of drug release were controlled by the loading drug and surfactant concentration. SLN system with effective drug loading efficiency and proper particle size for the intravenous or oral formulation can be prepared by selecting optimum drug and surfactant.

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Nanocellulose Applications for Drug Delivery: A Review

  • Lee, Seung-Hwan;Kim, Hyun-Ji;Kim, Jin-Chul
    • Journal of Forest and Environmental Science
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    • v.35 no.3
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    • pp.141-149
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    • 2019
  • Nanocellulose, which can exist as either cellulose nanocrystals or cellulose nanofibrils, has been used as a biomaterial for drug delivery owing to its non-immunogenicity, biocompatibility, high specific area, good mechanical properties, and variability for chemical modification. Various water-soluble drugs can be bound to and released from nanocelluloses through electrostatic interactions. The high specific surface area of nanocellulose allows for high specific drug loading. Additionally, a broad spectrum of drugs can bind to nanocellulose after facile chemical modifications of its surface. Controlled release can be achieved for various pharmaceuticals when the nanocellulose surface is chemically modified or physically formulated in an adequate manner. This review summarizes the potential applications of nanocelluloses in drug delivery according to published studies on drug delivery systems.

Alginate/Carboxymethyl Scleroglucan Hydrogels for Controlled Release of Protein Drugs

  • Lee, Chang-Moon;Jeong, Hwan-Jeong;Kim, Dong-Woon;Lee, Ki-Young
    • Macromolecular Research
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    • v.16 no.5
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    • pp.429-433
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    • 2008
  • Alginate/carboxymethyl scleroglucan (CMSG) hydrogels were suggested as a novel carrier for the controlled release of protein drugs. The drug release characteristics of alginate hydrogels were improved by CMSG addition. Scleroglucan (Sclg) was carboxymethylated using monochloroacetic acid in aqueous alkaline medium. Alginate/CMSG hydrogels were prepared by dropping the mixture solution of alginate/CMSG into calcium chloride solution. The swelling behaviors and drug release characteristics of the hydrogels were investigated in the buffers of pH 1.2 or 7.4. As the CMSG content increased in the hydrogels, the swelling ratio of the alginate/CMSG hydrogel increased rapidly in the buffer of pH 7.4. At pH 1.2, however, the swelling ratio significantly decreased compared to that at pH 7.4. According to in vitro release tests, only 15% of ovalbumin, investigated as a model protein drug, was released from the alginate/CMSG hydrogels at pH 1.2 within 6 h. At pH 7.4, however, the drug release significantly increased due to the rapid swelling of the hydrogels. The release and swelling behaviors of the hydrogels could be controlled by changing the CMSG content in the hydrogels. These results supported the use of alginate/CMSG hydrogels as a suitable carrier for the controlled release of protein drugs in a pH responsive manner.

Controlled Release of Propranolol Hydrochloride(PPH) from PPH-Solid Dispersion System-Polyvinyl Alcohol Hydrogel Hollow Type Suppository (염산 프로프라놀롤-고체 분산계-폴리비닐알코올 하이드로겔 중공좌제로부터의 약물방출)

  • Chung, Jeen-Hoon;Lee, Jeong-Yeon;Ku, Young-Soon
    • Journal of Pharmaceutical Investigation
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    • v.26 no.4
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    • pp.299-308
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    • 1996
  • In order to develop the controlled release of a drug from the suppsitories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppository forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The polyvinyl alcohol(PVA) hydrogel as a base, and propranolol HCl(PPH) as a model drug were employed. In vitro drug dissolution studies showed that the dissolved amounts(%) of PPH from PPH-methylcellulose(MC)-SDS and PPH-ethylcellulose(EC)-SDS reached 100% and 63% in 4.5-hours, respectively. In the relative strength test for PVA hydrogel, PVA hydrogel became harder and more rigid when the number of freezing-thawing cycles and the ratio of PVA 2000 were increased. In vitro drug release profile revealed that the release rate(%) of PPH from PPH-EC-SDS and PPH-MC-SDS hollow type suppositories were sustained. The release amount(%) of PPH from PPH-EC-SDS hollow type suppositories was not affected by storage time, but since the use of hydrophilic MC made PPH diffuse into the hydrogel after it absorbed the water of base, the various release patterns were appeared as the storage time went by. In vivo absorption experiments with rabbits showed that PPH-EC-SDS(PPH : EC=1:3) hollow type suppository delayed the absorption of PPH, significantly. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH powder hollow type suppository were $196.37{\pm}5.63\;ng/ml$, 1105.26 ng/ml/min and 8.66 min, respectively. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH-EC-SDS(PPH : EC=1:3) were $91.30{\pm]14.14\;ng/ml$, 554.69 ng/ml/min, 235.99 min, respectively.

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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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A Novel Drug Delivery System Design for Meloxicam

  • Kim, Hyun-Jo;Lee, Il-Kyu
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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    • pp.151-155
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    • 2005
  • A drug delivery system(DDS) for practically insoluble meloxicam was developed and evaluated by dissolution study. A novel DDS is two layered system, where the first layer is consisted of gas-forming agent for an immediate release and the second layer is composed of metolose SR(HPMC) for sustained release. This bilayered tablets were manufactured by using manual single punch machine. The results of dissolution study showed an initial burst release followed by sustained release for the experimental period time. From a pharmaceutical point of view, the designed DDS for meloxicam would be informative system in terms of poorly soluble analgesic medicines.

Development of Specific organ targeting drug delivery system II : Physico-pharaceutical study on the crose-linked albumin microspheres containing cytarabine

  • Kim, Chong-Kook;Lee, Jin-Kyu;Lah, Woon-Lyong
    • Archives of Pharmacal Research
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    • v.9 no.1
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    • pp.39-43
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    • 1986
  • Bovine serum albumin microspheres containing cytarabine were prepared using cross-linking agent, formaldehyde. The shape and the size distribution of them were observed. The shape of them was spherical and the susrface was compact and smooth. The size distribution of them was affected by dispersion forces during emulsfication. The release of cytarabine from albumin microspheres was dependent upon cross-linking time, amount of cross-linking agent and drug/albumin ratio. However, the difference of drug release by the dispersion forces was not great. After release test, the shape of albumin microspheres was nonspherical and the albumin matrix seemed to be a little relaxed. The degradation tests of albumin microspheres by the proteolytic enzyme showed that albumin microspheres were progressively digested according to the cross-linking degree.

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Thermosensitive Chitosan as an Injectable Carrier for Local Drug Delivery

  • Bae Jin-Woo;Go Dong-Hyun;Park Ki-Dong;Lee Seung-Jin
    • Macromolecular Research
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    • v.14 no.4
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    • pp.461-465
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    • 2006
  • Two types of injectable system using thermosensitive chitosan (chitosan-g-NIPAAm), hydrogel and microparticles (MPs)-embedded hydrogel were developed as drug carriers for controlled release and their pharmaceutical potentials were investigated. 5-Fluorouracil (5-FU)-loaded, biodegradable PLGA MPs were prepared by a double emulsion method and then simply mixed with an aqueous solution of thermosensitive chitosan at room temperature. All 5-FU release rates from the hydrogel matrix were faster than bovine serum albumin (BSA), possibly due to the difference in the molecular weight of the drugs. The 5-FU release profile from MPs-embedded hydrogel was shown to reduce the burst effect and exhibit nearly zero-order release behavior from the beginning of each initial stage. Thus, these MPs-embedded hydrogels, as well as thermosensitive chitosan hydrogel, have promising potential as an injectable drug carrier for pharmaceutical applications.

Using Polypyrrole for Drug Delivery System (폴리피롤을 이용한 약물전달시스템)

  • Lee, Sang-Jo;Lee, Seung-Ki;Oh, Myung-Hwan;Park, Jung-Ho
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2002.11a
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    • pp.448-451
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    • 2002
  • The possibility of using polypyrrole as a drug delivery system(DDS) has been studied using indicate (Phenol red) and substance with therapeutic activity(Sodium salicylate). In aqueous solution, negative potential is applied to polypyrrole then anion(with therapeutic activity) of sodium salicylate is released by redox processes of polypyrrole. The release amount of anionic drugs from polypyrrole is measured by UV-visible spectrometer which can measure UV-absorbance of materials. Electrode area that use for release amount measurement is$50mm^{2}(5{\times}10mm)$,and thickness of polypyrrole membrane is $15{\mu}m$. DC 1V applied in saline solution, the release amount according to time increased gradually. In various electrode area, release amount of anionic drug is directly to electrode area.

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Hydrophilic Albumin Microspheres as Cytarabine Carriers

  • Kim, Chong-Kook;Chung, Myung-Hoa;Oh, Yu-Kyoung;Lah, Woon-Lyong
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.123-128
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    • 1993
  • The surface of cyarabine-entrapped albumin microspheres, the surface modified albumin microspheres hsowed remakably incrased hydrophilicity, good dispersability in aqueous medium and reduced aggregation during storage which met the requirements of injectable drug carriers in acqueous vehicle. In vitro cytarabine release from hydrophilic albumin microspheres (HAM) was a function of the cytarabine to albumin ratio, whereas no significant difference in the releasing capacity was obnserved between surface modified HAM within the small size range$(2\;to\;5\mu{m)}$ studied. HAM containing 15-23% drug were gradually degraded by protease and continuously released up to 60% of the total entrapped cytarabine for 6h. These results thus suggest that HAM is a suitable cytarabine carrier which may be injected intraveneously with the benefits of a reduced risk of blood embolism induced by aggregates and prolonged cytarabine release.

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