• Title/Summary/Keyword: Drug carriers

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Nano-sized Drug Carriers and Key Factors for Lymphatic Delivery

  • Choi, Ji-Hoon;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.75-82
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    • 2010
  • Specific diseases like cancer and acquired immune deficiency syndrome (AIDS) occur at various organs including lymphatics and spread through lymphatic system. Thus, if therapeutic agents for such diseases are more distributed or targeted to lymphatic system, we can obtain several advantages like reduction of systemic side effect and increase of efficacy. For these reasons, much interest has been focused on the nature of lymphatics and a lot of studies for lymphatic delivery of drugs have been carried out. Because lymphatics consist of single layer endothelium and have high permeability compared with blood capillaries, especially, the studies using nano-sized carriers have been performed. Polymeric nano-particle, liposome, and lipid-based vehicle have been adopted for lymphatic delivery as carriers. According to the administration route and the kind of carrier, the extent of lymphatic delivery efficiency of nano-sized carriers has been changed and influenced by several factors such as size, charge, hydrophobicity and surface feature of carrier. In this review, we summarized the key factors which affect lymphatic uptake and the major features of carriers for achieving the lymphatic delivery. Lymphatic delivery of drug using nano-sized carriers has many fold improved ability of lymphatic delivery compared with that of conventional dosage forms, but it has not shown whole lymph selectivity yet. Even though nano-sized carriers still have the potential and worth to study as lymphatic drug delivery technology as before, full understanding of delivery mechanism and influencing factors, and setting of pharmacokinetic model are required for more ideal lymphatic delivery of drug.

Stereocomplex Poly(lactic acid) Discoidal Microparticles for Sustained Drug Release (약물지연방출을 위한 스테레오컴플렉스 PLA 원반형 마이크로입자)

  • Park, Chaewon;Park, Sanghyo;Kim, Woo Cheol;Key, Jaehong
    • Journal of Biomedical Engineering Research
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    • v.41 no.1
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    • pp.62-66
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    • 2020
  • Controlled drug release is important for effective treatment of cancer. Poly(DL-lactide-co-glycolide) acid (PLGA) is a Food and Drug Administration (FDA) approved polymer and have been extensively studied as drug delivery carriers with biodegradable and biocompatible properties. However, PLGA drug delivery carriers are limited due to the initial burst release of drug. Certain drugs require an early rapid release, but in many cases the initial rapid release can be inefficient, reducing therapeutic effects and also increasing side effects. Therefore, sustained release is important for effective treatment. Poly Lactic Acid stereo complex (PLA SC) is resistant to hydrolysis and has high stability in aqueous solutions. Therefore, in this work, PLGA based discoidal polymeric particles are modified by Poly Lactic Acid stereocomplex (PLAsc DPPs). PLAsc DPPs are 3 ㎛ in diameter, also showing a relatively sustained release profile. Fluorescein 5(6)-isothiocyanate (FITC) released from PLAsc DPPs was continuously observed until 38 days, which showed the initial release of FITC from PLAsc DPPs was about 3.9-fold reduced as compared to PLGA based DPPs at 1 hour.

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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Folate-Targeted Nanostructured Lipid Carriers (NLCs) Enhance (Letrozol) Efficacy in MCF-7 Breast Cancer Cells

  • Sabzichi, Mehdi;Mohammadian, Jamal;Khosroushahi, Ahmad Yari;Bazzaz, Roya;Hamishehkar, Hamed
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.12
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    • pp.5185-5188
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    • 2016
  • Objective: Targeted-drug-delivery based lipid nanoparticles has emerged as a new and effective approach in cancer chemotherapy. Here, we investigated the ability of folate-modified nanostructured lipid carriers (NLCs) to enhance letrozol (LTZ) efficacy in MCF-7 breast cancer cells. Methods: New formulations were evaluated regarding to particle size and scanning electron microscope (SEM) features. Anti-proliferative effects of LTZ loaded nanoparticles were examined by MTT assay. To understand molecular mechanisms of apoptosis and cell cycle progression, flow cytometric assays were applied. Results: Optimum size of nanoparticles was obtained in mean average of $98{\pm}7nm$ with a poly dispersity index (PDI) of 0.165. The IC50 value was achieved for LTZ was $2.2{\pm}0.2{\mu}M$. Folate-NLC-LTZ increased the percentage of apoptotic cells from 24.6% to 42.2% compared LTZ alone (p<0.05). Furthermore, LTZ loaded folate targeted NLCs caused marked accumulation of cells in the subG1 phase. Conclusion: Taken together, our results concluded that folate targeted LTZ can be considered as potential delivery system which may overcome limitations of clinical application of LTZ and improve drug efficacy in tumor tissue.

Application of sickle red blood cells for targeted cancer therapy (항암치료를 위한 겸형적혈구의 응용)

  • Choe, Se-woon
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • 2016.05a
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    • pp.715-717
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    • 2016
  • Conventional drug carriers such as liposomes, nanoparticles, polymer micelles, polymeric conjugate and lipid microemulsion for cancer chemotherapy shield normal tissues from toxic drugs to treat cancer cells in tumors. However, inaccurate tumor targeting uncontrolled drug release from the carriers and unwanted accumulation in healthy sites can limit treatment efficacy with current conventional drug carriers with insufficient concentrations of drugs in the tumors and unexpected side effects as a result. In this research, we examined the use of sickle red blood cells as a new drug carrier with novel tumor targeting and controlled release properties. Sickle red blood cells show natural tumor preferential accumulation without any manipulation and controlled drug release is possible using a hemolysis method with photosensitizers.

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Drug-release Properties of Double-layered Microspherical Carriers which Consist of Outer Shell of Poly(D,L-lactide) and Inner Core of Alginate or Chitosan (Poly(D,L-lactide)를 외부 껍질로 하고 Alginate 또는 Chitosan을 내부 코어로 구성한 이중미립구 담체의 약물방출 특성)

  • Kim, Ja Won;Song, Min Jeong;Lee, Sang Min;Lim, So Ryong;Jung, Su Jin;Kim, Hong Sung
    • Polymer(Korea)
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    • v.36 no.6
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    • pp.699-704
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    • 2012
  • Double-layered polymeric carrier was designed for release control of hydrophilic drug in oral administration. Biopolymeric chitosan and alginate were examined as polar absorbents, poly(D,L-lactide) as a hydrophobic shell, and theophylline and diclofenac sodium as loading drugs. The fabrication of the carriers was prepared in the form of double-layered microsphere for delayed and successively extended release, which consisted of outer shell of poly(D,L-lactide) and inner core of alginate or chitosan with drugs. Morphologies and drug-release behaviors of the carriers were investigated, which were influenced by a combination of polarity between carrier and drug. It was confirmed that the relative polarities of the carriers, the drugs, and the environmental pH affected significantly the drug-release property.

Photoresponsive Nanocontainers with Ordered Porous Channels

  • Cho, Wansu;Kwon, Youngje;Park, Chiyoung
    • Elastomers and Composites
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    • v.54 no.2
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    • pp.149-155
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    • 2019
  • Controlled mass transport in response to stimuli is essential for drug carriers. The complexity of the signaling system under physiological conditions has led researchers to develop precise nanocontainers that respond to stimuli in the physiological environment. Owing to several reasons, soft nanocontainers such as liposomes and micelles have been investigated for use as drug delivery systems. However, such carriers often suffer from the undesired leakage of drug molecules. In contrast, inorganic nanocontainers are robust, and their surfaces can be easily functionalized. For example, mesoporous silica nanoparticles equipped with gatekeeper molecules are increasingly being used for the controlled release of drug molecules in response to the desired stimuli. Since the development of the first hybrid nanocontainer comprising molecular machines, multiple versions of such gatekeeper systems featuring significantly improved stability and precise response to stimuli have been reported. In this study, various methods for incorporating photoresponsive nanocontainers with porous channels are developed.

In vitro release test models for water-insoluble drugs loaded in colloidal carriers

  • Lee, Jung-Min;Choi, Sung-Up;Lee, Byoung-Moo;Lee, Sung-Jae;Choi, Young-Wook
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.295.1-295.1
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    • 2003
  • A suitable model for the estimation of the drug release from nanoparticles has been varied and problematic, especially for the release from lipid nanoparticles containing water-insoluble drugs, due to the difficult particle collection from the release medium. Dialysis membrane has been widely used for the release test from colloidal carrier systems. The amount of drug from the carriers in normal dialysis diffusion technique was very low typically. (omitted)

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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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Investigation of Tacrolimus Loaded Nanostructured Lipid Carriers for Topical Drug Delivery

  • Nam, So-Hee;Ji, Xu Ying;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.956-960
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    • 2011
  • The objective of this investigation was to develop nanostructured lipid carriers (NLCs) of tacrolimus by the hot homogenization technique by sonication. NLCs are commonly prepared by emulsification and lyophilization. The feasibility of fabricating tacrolimus-loaded NLCs was successfully demonstrated in this study. The developed NLCs were characterized in terms of their particle size, zeta potential, entrapment efficiency (EE) of tacrolimus, and morphology. Studies were conducted to evaluate the effectiveness of the NLCs in improving the penetration rate through hairless mouse skin. Tacrolimus-loaded NLCs were found to have an average size of $123.4{\pm}0.3\;nm$, a zeta potential of $-24.3{\pm}6.2\;mV$, and an EE of 50%. In vitro penetration tests revealed that the tacrolimus-loaded NLCs have a penetration rate that is 1.64 times that of the commercial tacrolimus ointment, Protopic$^{(R)}$.