• Title/Summary/Keyword: drug design

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Layer-by-layer assembled polymeric thin films as prospective drug delivery carriers: design and applications

  • Park, Sohyeon;Han, Uiyoung;Choi, Daheui;Hong, Jinkee
    • Biomaterials Research
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    • v.22 no.4
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    • pp.290-302
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    • 2018
  • Background: The main purpose of drug delivery systems is to deliver the drugs at the appropriate concentration to the precise target site. Recently, the application of a thin film in the field of drug delivery has gained increasing interest because of its ability to safely load drugs and to release the drug in a controlled manner, which improves drug efficacy. Drug loading by the thin film can be done in various ways, depending on type of the drug, the area of exposure, and the purpose of drug delivery. Main text: This review summarizes the various methods used for preparing thin films with drugs via Layer-by-layer (LbL) assembly. Furthermore, additional functionalities of thin films using surface modification in drug delivery are briefly discussed. There are three types of methods for preparing a drug-carrying multilayered film using LbL assembly. First methods include approaches for direct loading of the drug into the pre-fabricated multilayer film. Second methods are preparing thin films using drugs as building blocks. Thirdly, the drugs are incorporated in the cargo so that the cargo itself can be used as the materials of the film. Conclusion: The appropriate designs of the drug-loaded film were produced in consideration of the release amounts and site of the desired drug. Furthermore, additional surface modification using the LbL technique enabled the preparation of effective drug delivery carriers with improved targeting effect. Therefore, the multilayer thin films fabricated by the LbL technique are a promising candidate for an ideal drug delivery system and the development possibilities of this technology are infinite.

Property-based Design of Ion-Channel-Targeted Library

  • Ahn, Ji-Young;Nam, Ky-Youb;Chang, Byung-Ha;Yoon, Jeong-Hyeok;Cho, Seung-Joo;Koh, Hun-Yeong;No, Kyoung-Tai
    • Proceedings of the Korean Society for Bioinformatics Conference
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    • 2005.09a
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    • pp.134-138
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    • 2005
  • The design of ion channel targeted library is a valuable methodology that can aid in the selection and prioritization of potential ion channel-likeness for ion-channel-targeted bio-screening from large commercial available chemical pool. The differences of property profiling between the 93 ion-channel active compounds from MDDR and CMC database and the ACDSC compounds were classified by suitable descriptors calculated with preADME software. Through the PCA, clustering, and similarity analysis, the compounds capable of ion channel activity were defined in ACDSC compounds pool. The designed library showed a tendency to follow the property profile of ion-channel active compounds and can be implemented with great time and economical efficiencies of ligand-based drug design or virtual high throughput screening from an enormous small molecule space.

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Drug Targeting to Lungs by Way of Microspheres

  • Harsha, N. Sree;Rani, R.H. Shobha
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.598-604
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    • 2006
  • In many conventional drug delivery systems in vogue, failure to deliver efficient drug delivery at the target site/organs; is evident as a result, less efficacious pharmacological response is elicited. Microspheres can be derived a remedial measure which can improve site-specific drug delivery to a considerable extent. As an application, Lung-targeting Ofloxacin-loaded gelatin microspheres (GLOME) were prepared by water in oil emulsion method. The Central Composite Design (CCD) was used to optimize the process of preparation, the appearance and size distribution were examined by scanning electron microscopy, the aspects such as in vitro release characteristics, stability, drug loading, loading efficiency, pharmacokinetics and tissue distribution in albino mice were studied. The experimental results showed that the microspheres in the range of $0.32-22\;{\mu}m$. The drug loading and loading efficiency were 61.05 and 91.55% respectively. The in vitro release profile of the microspheres matched the korsmeyer’s peppas release pattern, and release at 1h was 42%, while for the original drug, ofloxacin under the same conditions 90.02% released in the first half an hour. After i.v. administration (15 min), the drug concentration of microspheres group in lung in albino mice was $1048\;{\mu}g/g$, while that of controlled group was $6.77\;{\mu}g/g$. GLOME found to release the drug to a maximum extent in the target tissue, lungs.

Bioequivalence Study of Loxoprofen Sodium in healthy Volunteers (Loxoprofen sodium 제제(레녹스정)의 생물학적 동등성시험)

  • 최주영;유내춘;박민수;김경환
    • Biomolecules & Therapeutics
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    • v.6 no.4
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    • pp.417-422
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    • 1998
  • Loxoprofen sodium (sodium 2-[4-(2-oxocyclopentylmethyl)phenyl] propionate dehydrate) is a nonsteroidal antiinflammatory drug of $\alpha$-phenyl propionic acid derivative. To test the bioequivalence of loxoprofen, the pharmacokinetic parameters of new preparation of loxoprofen, LENOX was compared with LOXONIN as a reference drug. Fourteen healthy volunteers were entered to the stydy (Yonsei University College of Medicine, Severance Hospital IRB approval No. 9608). They were administered 60 mg of loxoprofen in 2$\times$2 cross-over design. There was one week of drug-free interval between doses. The blood sample was taken on schedule up to 8 hours, and the plasma concentration loxoprofen was measured by reverse phase high-performance liquid chromatography (HPLC) with UV-detector. There were no significant difference between two preparations when AUC, Cmax, and Tmax were compared by ANOVA. The mean differences of AUC, Cmax, and Tmax were within 20% of the reference drug: the values were 2.22,5.61, and 12.50%, respectively. The confidence limits of AUC and Cmax but not Tmax satisfied the bioequivalence criteria. These results suggest that the tested LENOX is bioequivalent to the reference drug.

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A Novel Drug Delivery Approach to Olanzapine Orally Dispersible Tablet (ODT) in the Phase of Schizophrenia and Its Pharmacokinetics

  • Kim, Hyun-Jo;Park, Jeong-Hwan
    • Journal of Pharmaceutical Investigation
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    • v.40 no.5
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    • pp.297-304
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    • 2010
  • The present work focuses on preparation of olanzapine, orally dispersing tablets by direct compression method. Effect of super disintegrant crospovidone, disintegration time, drug content on in vitro release has been studied. A factorial design was employed in formulating a prompt dispersible tablet. The selected independent variables crospovidone and fmelt showed significant effect on dependent variables i.e. disintegration time and percent drug dissolved. Disintegration time and percent drug dissolved decreased with increase in the level of crospovidone. The similarity factor $f_2$ was found to be 97.48 for the developed formulation indicating the release was similar to that of the marketed formulation. Pharmacokinetics of olanzapine after single-dose oral administration of orally disintegrating tablet in normal volunteers were evaluated and the results showed that PK parameters (Cmax, Tmax, AUC) of the designed ODT matrix were similar to those of commercial product, Zyprexa Zydis$^{(R)}$ as a reference.

Design of Oral Patches for the Treatment of Aphthous Stomatitis : Drug Layer (아프타성 구내염 치료용 구강 패취의 설계 : 약물층)

  • Lee, Kyu-Hyun;Park, Eun-Seok;Chi, Sang-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.25 no.4
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    • pp.339-345
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    • 1995
  • For the effective treatment of aphthous stomatitis, the matrix type mucoadhesive patches containing triamcinolone acetonide have been formulated. The drug layer was obtained by drying the polymer gel which was prepared with carbomer 934P, ammoniomethacrylate copolymer, titanium dioxide and polyethylene glycol 400. The effects of the content of additives on physical characteristics of the polymer gel and the drug layer were evaluated. The addition of carbomer increased the yield point and the zero-shear viscosity of polymer gel as well as the thickness, the water absorption ratio, the adhesive time and $T_{50%}$ of drug layer. The adhesive time and the water absorption ratio of drug layer were also improved by the addition of ammoniomethacrylate copolymer, but the addition of titanium dioxide had decreased the zero-shear viscosity of polymer gel and the adhesive time of drug layer.

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Design and Synthesis of Novel Antidiabetic Agents

  • Lee Joon Yeol;Park Won-Hui;Cho Min-Kyoung;Yun Hyun Jin;Chung Byung-Ho;Pak Youngmi Kim;Hahn Hoh-Gyu;Cheon Seung Hoon
    • Archives of Pharmacal Research
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    • v.28 no.2
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    • pp.142-150
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    • 2005
  • The synthesis and structure-activity relationships of a novel series of substituted quercetins that activates peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) are reported. The $PPAR{\gamma}$ agonistic activity of the most potent compound in this series is comparable to that of the thiazolidinedione-based antidiabetic drugs currently in clinical use.

Development and Application of Detection Method for Aphanizomenon flos-aquae not Usable as a Food Materials in Korea (식품 중 사용금지 원료인 Aphanizomenon flos-aquae 검출법 개발 및 응용)

  • Park, Yong-Chjun;Shin, Seung-Jung;Lee, Ho-Yeon;Kim, Yong-Sang;Kim, Mi-Ra;Lee, Sang-Jae;Lee, Hwa-Jung
    • Journal of Food Hygiene and Safety
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    • v.28 no.2
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    • pp.188-193
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    • 2013
  • Anatoxin-a, saxitoxin and neosaxitoxin are produced by Aphanizomenon flos-aquae that is a sort of the cyanobacteria phylum. Therefore, it is not permitted for food materials in Korea. Traditionally, the classification of cyanobacteria has been based on morphological characters such as trichome width, cell size, division planes, shape, and the presence of character such as gas vacuole. But, some diagnostic features, such as gas vacuole or akinetes, can show variation with different environmental or growth conditions and even be lost during cultivation. Therefore, we developed detection method for functional foods containing Aph. flos-aquae by PCR. To design the primer, 16S rRNA region of Aph. flos-aquae, Spirulina laxissima, and Spirulina spp. registered in the GeneBank (www.ncbi.nlm.nih.gov) have been used and for comparative analysis, BioEdit ver. 7.0.9.0. was used. As a result, we was design AFA-F1/AFA-R1 (363 bp) primer for the differentiation Aph. flos-aquae from chlorella, spirulina, green tea, and spinach. Also, it could be distinguished chlorella and spirulina products those are made to contain 1% Aph. flos-aquae.

Development of Detection Method for Oilfish (Ruvettus pretiosus and Lepidocybirium flavobrunneum) as a Food Materials not Usable in Foods (식품원료로 사용금지 대상인 기름치 (기름갈치꼬치 및 흑갈치꼬치) 판별법 개발)

  • Park, Yong-Chjun;Kim, Mi-Ra;Jung, Yong-Hyun;Shin, Joon-Ho;Kim, Kyu-Heon;Lee, Jae-Hwang;Cho, Tae-Yong;Lee, Hwa-Jung;Lee, Sang-Jae;Han, Sang-Bae
    • Journal of Food Hygiene and Safety
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    • v.28 no.1
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    • pp.50-55
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    • 2013
  • Since 1 June 2012, it is prohibited to sell oilfish as a food material but there are still many illegal cases of selling oilfish as if it is tuna or grilled Patagonian toothfish. So it is absolutely crucial to construct the system to distinguish the real food material from oilfish. There are two sorts of oil fish called Ruvettus pretiosus and Lepidocybirium flavobrunneum involved in Percifomes order and Gempylidae class. 16S DNA gene region in mitochondria was selected to design the specific primers. For design species-specific primer, the theoretical experiment were performed for the sequences of R. pretiosus, L. flavobrunneum, Thunnus thynnus, Thunnus albacores, Makaira mitsukurii and Xiphias gladius, registered at the Gene bank from the National Centre for Biotechnology Information, using BioEdit 7.0.9.0. program. Through the analysis of the result from experiments, it was possible to design the 4 kinds of primers to distinguish R. pretiosus and L. flavobrunneum. As a comparison group, 3 kinds of tuna and 4 kinds of billfishes were selected and experimental verification was performed. As a result, for R. pretiosus and L. flavobrunneum, R.P-16S-006-F/R.P-16S-008-R and L.F-16S-004-F/L.F-16S-006-R primers were selected eventually and PCR condition was established. In addition, 178bp and 238bp of PCR products were confirmed from the established condition and non-specific band was not amplified among similar species. Therefore, the species-specific primers developed in this study would be very useful and used in various ways such as internet shopping mall and illegal distributions with fast and scientific results.

A Prediction Model of Drug Misuse Behaviors in Community-Dwelling Older Adults (재가노인의 약물오용행위 예측모형)

  • Hong, Se Hwa;Yoo, Kwang Soo
    • Journal of Korean Academy of Nursing
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    • v.46 no.5
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    • pp.630-641
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    • 2016
  • Purpose: This study was designed to construct a model which explains drug misuse behaviors in community-dwelling older adults. Methods: The design of this research is a cross-sectional study using structure equation modeling. The hypothetical model consisted of two types of variables: the exogenous variables of health status, cognitive ability, and negative emotion, and the endogenous variables of number of drugs, and drug misuse behaviors. The data collection was conducted from September 2 to September 21, 2013 through self-report questionnaires. Participants were 320 community-dwelling adults over the age of 65 living in J city. Data were analyzed with SPSS 21.0 program and Amos 18.0 program. Results: The results of the model fitness analysis were satisfied. The predictor variables for the hypothetical model explained 62.3% of variance regarding drug misuse behaviors. Drug misuse behaviors were directly affected by health status, cognitive ability, negative emotion and number of drugs and indirectly affected by health status, and negative emotion through number of drugs. Conclusion: These findings indicate factors that should be used in developing effective nursing interventions for safe and proper drug use and the prevention of drug misuse behaviors in community-dwelling older adults.