• Title/Summary/Keyword: Drug delivery systems

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Preparation and Characterization of Cellulose Nanocrystals Reinforced Poly (vinyl alcohol) Based Hydrogels for Drug Delivery System (약물 전달 시스템 적용을 위한 셀룰로오스 나노크리스탈(CNCs) 강화 Poly(vinyl alcohol) 기반 하이드로겔의 제조 및 특성)

  • CHO, Hyejung;YOO, Won-Jae;AHN, Jinsoo;CHUN, Sang-Jin;LEE, Sun-Young;GWON, Jaegyoung
    • Journal of the Korean Wood Science and Technology
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    • v.48 no.4
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    • pp.431-449
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    • 2020
  • Structural property of most hydrogels is soft, resulting in low mechanical performance that limits their usage in the biomedical applications. For overcoming the drawback, cellulose nanocrystals (CNCs) were adopted in this study. Effects of CNCs on characteristics and drug delivery performance of poly (vinyl alcohol) based hydrogels were explored. FT-IR results showed that the fabricated hydrogels had semi-IPN (semi-interpenetrating polymer network) by formation of acetal and aldehyde bridge. Water absorption and swelling ratio decreased with increasing CNCs content, and the hydrogels with CNCs showed better viscoelastic performance than the without CNCs. Also, CNCs mostly improved the ability of the hydrogel to absorb the drug and the sustainability of the drug release. These results demonstrated that incorporating CNCs into the hydrogel systems can be a good alternative to improve drug delivery performance and mechanical property of the hydrogels.

A Formulation Study for the Controled Release Rate of Diltiazem. HCl using the Multiple Drug Release System (다중약물방출시스템을 이용한 염산딜티아젬의 방출속도 조절에 관한 연구)

  • Kim, Hak-Hyung;Oh, Jin-Hwan;Han, Kun
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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    • pp.157-163
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    • 2005
  • The pellets with multiple drug release system (MDRS) of Diltiazem. HCl which consist of immediate drug release layer, drug reservoir layer and controlled release rate membrane, were prepared by using CF-Coater. As main factors for more effective MDRS of Diltiazem. HCl, ethylcellulose was used for the controlling drug release rate, and diethylphthalate was used for plasticizer, respectively. In vitro evaluation study was performed by comparative dissolution test between our test MDRS and reference Diltiazem. HCl preparation. The physical tests were performed using FT-IR and SEM. In vivo evaluation was also performed by observing the behavior of a plasma drug concentration after oral administration. The bioavailability was determined by analyzing the blood sample after oral administration to healthy, male volunteers once a day. As a result, there were no significant differences in bioequivalence parameters $(AUC_{\infty},\;C_{max},\;t_{1/2})$ between two systems. It might be concluded that our MDRS of Diltiazem. HCl could be an alternative delivery system to reference drug preparation.

Laser-assisted Delivery of a Combined Antioxidant Formulation Enhances the Clinical Efficacy of Fractional Microneedle Radiofrequency Treatment: A Pilot Study

  • Kim, Jihee;Kim, Soo Min;Jung, Bok Ki;Oh, Sang Ho;Kim, Young-Koo;Lee, Ju Hee
    • Medical Lasers
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    • v.10 no.3
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    • pp.161-169
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    • 2021
  • Background and Objectives Fractional microneedle radiofrequency systems are popular options to increase elasticity in aging skin. Laser-assisted drug delivery is a promising method for the epidermal injection of topically applied drugs and cosmetic ingredients. This study assesses the safety and efficacy of topical delivery of L-ascorbic acid, vitamin E, and ferulic acid after fractional microneedle radiofrequency treatment for reducing photodamage. Materials and Methods In this prospective, single-center, split-face, controlled pilot study, six women (mean age, 48.0 years; range, 35-57 years; Fitzpatrick skin types III and IV) exhibiting mild to moderate photodamage, underwent a single session of fractional microneedle radiofrequency treatment. The patients were instructed to apply the antioxidant formulation to only one side of the face. Patients were evaluated 3 days, 7 days, and 4 weeks thereafter, using three-dimensional imaging and ultrasound. Ex vivo, the full-thickness human skin was used for molecular and histological evaluation. Statistical analysis was achieved by applying t-tests, Mann-Whitney U tests, and one-way analyses of variance. Results Compared to the untreated side, the antioxidant-treated side exhibited a significant increase in dermal thickness (10.32% vs. 17.54%, p < 0.05), but not in skin elasticity (4.76% vs. 4.69%, p > 0.05). The difference in erythema between the sides was statistically not significant (p > 0.05). In the ex vivo model, expression of FGF2 in the skin was significantly increased after application of the antioxidant formulation, as compared to results obtained subsequent to fractional microneedle radiofrequency treatment only (p < 0.01). Conclusion This study demonstrates that for the treatment of photodamaged skin, laser-assisted delivery of the antioxidant formulation is a safe and effective adjuvant modality following fractional microneedle radiofrequency.

The Effect of Enhancer on the Penetration of Indapamide through Hairless Mouse Skin (경피흡수촉진제의 영향에 따른 인다파마이드의 피부투과)

  • Seo, Hui;Jeung, Sang-Young;Park, Ji-Seon;Shin, Byung-Cheol;Hwang, Sung-Joo;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.237-242
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    • 2007
  • The chemical formula of indapamide is 3-(aminosulfonyl)-4-chloro-N-(2,3-dihydro-2-methyl-1H-indol-l-yl)-benzamide, Indapamide is an oral antipertensive diuretic agent indicated for the treatment of hypertensive and edema. Indapamide inhibits carbonic anhydrase enzyme. Transdermal drug delivery systems, as compared to their corresponding classical oral or injectable dosage form counterparts, offer many advantages. The most important advantages are improved systemic bioavailability of the pharmaceutical active ingredients (PAI), because the first-pass metabolism by the liver and digestive system are avoided; and the controlled, constant drug delivery profile (that is, controlled zero-order absorption). Also of importance is the reduced dose frequency compared to the conventional oral dosage forms (that is, once-a-day, twice-a-week or once-a-week). Other benefits include longer duration of therapeutic action from a single application, and reversible action. For example, patches can be removed to reverse any adverse effects that may be caused by overdosing. In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of Indapamide, the skin permeation rates of Indapamide from vehicles of different composition were determined using Franz cells fitted with excised hairless skins. Solubility of Indapamide in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of Indapamide, The solvents used were Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol. Lauroglycol90 increase the permeability of indapamide approximately 3.75-fold compared with the control. Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol showed flux of $0.06ug/cm^2/hr,\;0.4ug/cm^2/hr,\;0.21ug/cm^2/hr,\;0.72ug/cm^2/hr,\;0.29ug/cm^2/hr$, respectively.

Drug Target Identification and Elucidation of Natural Inhibitors for Bordetella petrii: An In Silico Study

  • Rath, Surya Narayan;Ray, Manisha;Pattnaik, Animesh;Pradhan, Sukanta Kumar
    • Genomics & Informatics
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    • v.14 no.4
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    • pp.241-254
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    • 2016
  • Environmental microbes like Bordetella petrii has been established as a causative agent for various infectious diseases in human. Again, development of drug resistance in B. petrii challenged to combat against the infection. Identification of potential drug target and proposing a novel lead compound against the pathogen has a great aid and value. In this study, bioinformatics tools and technology have been applied to suggest a potential drug target by screening the proteome information of B. petrii DSM 12804 (accession No. PRJNA28135) from genome database of National Centre for Biotechnology information. In this regards, the inhibitory effect of nine natural compounds like ajoene (Allium sativum), allicin (A. sativum), cinnamaldehyde (Cinnamomum cassia), curcumin (Curcuma longa), gallotannin (active component of green tea and red wine), isoorientin (Anthopterus wardii), isovitexin (A. wardii), neral (Melissa officinalis), and vitexin (A. wardii) have been acknowledged with anti-bacterial properties and hence tested against identified drug target of B. petrii by implicating computational approach. The in silico studies revealed the hypothesis that lpxD could be a potential drug target and with recommendation of a strong inhibitory effect of selected natural compounds against infection caused due to B. petrii, would be further validated through in vitro experiments.

Development of Solid Self-nanoemulsifying Drug Delivery Systems of Ticagrelor Using Porous Carriers (다공성의 캐리어를 이용한 티카그렐러 함유 고형의 자가 나노유화 약물전달시스템 개발)

  • Choi, Hyung Joo;Kim, Kyeong Soo
    • Journal of Life Science
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    • v.31 no.5
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    • pp.502-510
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    • 2021
  • The objective of this study was to develop a novel ticagrelor-loaded self-nanoemulsifying drug delivery system with an enhanced solubility and dissolution rate. Numerous oils and surfactants were screened, then medium chain triglyceride (MCT) oil and the surfactants polyoxyethylene sorbitan monooleate (Tween 80) and Labrafil M1944CS were selected for the preparation of the ticagrelor-loaded self-nanoemulsifying drug delivery system. A pseudo-ternary phase diagram was constructed to detect the nanoemulsion region. Of the various formulations tested, the liquid SNEDDS, composed of MCT (oil), Tween 80 (surfactant), and Labrafil M1944CS (cosurfactant) at a weight ratio of 20/70/10 produced the smallest emulsion droplet size (around 20.56±0.70 nm). Then, particle size, polydispersity, and zeta potential were measured using drugs containing liquid SNEDDS. The selected ticagrelor-loaded liquid SNEDDS was spray-dried to convert it into a ticagrelor-loaded solid SNEDDS with a suitable inert carrier, such as silicon dioxide, calcium silicate, or magnesium aluminometasilicate. The solid SNEDDS was characterized by scanning electron microscopy, transmission electron microscopy, and in vitro dissolution studies. SEM, PXRD, and DSC results suggested that amorphous ticagrelor was present in the solid SNEDDS. Also, the solid SNEDDS significantly increased the dissolution rate of ticagrelor. In particular, the emulsion particle size and the polydispersity index of the solid SNEDDS using silicon dioxide (SS1) as a carrier was the smallest among the evaluated solid SNEDDS, and the flowability and compressibility result of the SS1 was the most suitable for the manufacturing of solid dosage forms. Therefore, solid SNEDDS using silicon dioxide (SS1) could be a potential nano-sized drug delivery system for the poorly water-soluble drug ticagrelor.

Preparation of PNIPAM Hydrogel Containing Lipoic Acid (리포익산을 함유한 PNIPAM 하이드로젤의 제조)

  • Yoon, Hye-Ri;Lee, Jong-Hwi
    • Polymer(Korea)
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    • v.36 no.4
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    • pp.455-460
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    • 2012
  • Poly(N-isopropylacrylamide) (PNIPAM) hydrogel has been studied as an important drug delivery system due to its volume transition or temperature-responsive swelling properties, whose phase separation temperature is similar to the body temperature. However, because of hydrophilic PNIPAM, hydrophobic drugs are difficult to be uniformly loaded in the networks. Antioxidant alpha-lipoic acid (LA) can be prepared as a polymer(polylipoic acid, PLA) by ring opening polymerization, which is hardly developed as a material due to its low molecular weight and easy depolymerization. To overcome this limitation, a hydrophobic active ingredient, LA was reacted with NIPAM into stable hydrogels. Simple thermal radical reaction successfully resulted in a hydrogel (PNIPAM/PLA), which was confirmed by DSC, FTIR, and Raman spectroscopy. The PNIPAM/PLA showed temperature-responsive properties, and their volume swelling decreased with an increase in lipoic acid content. These hydrogels can carry hydrophobic drugs with PNIPAM and the hydrogels could be useful as final drug delivery systems having lipoic acid as an antioxidant.

Sequential anti-inflammatory and osteogenic effects of a dual drug delivery scaffold loaded with parthenolide and naringin in periodontitis

  • Rui Chen;Mengting Wang;Qiaoling Qi;Yanli Tang;Zhenzhao Guo;Shuai Wu;Qiyan Li
    • Journal of Periodontal and Implant Science
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    • v.53 no.1
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    • pp.20-37
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    • 2023
  • Purpose: Our pilot study showed that a 3-dimensional dual drug delivery scaffold (DDDS) loaded with Chinese herbs significantly increased the regenerated bone volume fraction. This study aimed to confirm the synergistic anti-inflammatory and osteogenic preclinical effects of this system. Methods: The targets and pathways of parthenolide and naringin were predicted. Three cell models were used to assess the anti-inflammatory effects of parthenolide and the osteogenic effects of naringin. First, the distance between the cementoenamel junction and alveolar bone crest (CEJ-ABC) and the bone mineral density (BMD) of surgical defects were measured in a rat model of periodontitis with periodontal fenestration defects. Additionally, the mRNA expression levels of matrix metallopeptidase 9 (MMP9) and alkaline phosphatase (ALP) were measured. Furthermore, the number of inflammatory cells and osteoclasts, as well as the protein expression levels of tumor necrosis factor-alpha (TNF-α) and levels of ALP were determined. Results: Target prediction suggested prostaglandin peroxidase synthase (PTGS2) as a potential target of parthenolide, while cytochrome P450 family 19 subfamily A1 (CYP19A1) and taste 2 receptor member 31 (TAS2R31) were potential targets of naringin. Parthenolide mainly targeted inflammation-related pathways, while naringin participated in steroid hormone synthesis and taste transduction. In vitro experiments revealed significant antiinflammatory effects of parthenolide on RAW264.7 cells, and significant osteogenic effects of naringin on bone marrow mesenchymal stem cells and MC3T3-E1 cells. DDDS loaded with parthenolide and naringin decreased the CEJ-ABC distance and increased BMD and ALP levels in a time-dependent manner. Inflammation was significantly alleviated after 14 days of DDDS treatment. Additionally, after 56 days, the DDDS group exhibited the highest BMD and ALP levels. Conclusions: DDDS loaded with parthenolide and naringin in a rat model achieved significant synergistic anti-inflammatory and osteogenic effects, providing powerful preclinical evidence.

Self-organized Nanogels of Polysaccharide Derivatives in Anti-Cancer Drug Delivery

  • Park, Sin-Jung;Na, Kun
    • Journal of Pharmaceutical Investigation
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    • v.40 no.4
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    • pp.201-212
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    • 2010
  • Self-organized nanogels from polysaccharide derivatives offer a promising approach in treatment of cancer due to their flexibility in chemistry and their ability to improve the therapeutic index of a drug by modifying biodistribution by their preferential localization at target sites and lower distribution in normal healthy tissues. These properties have promoted studies of active cancer targeting by self-organized nanogels for even better accumulation in solid tumors. However although many researchers have reported their potential by using cell culture systems and small animal tumor models in cancer therapy, these nanogels need more decoration such as conjugation with targeting moiety and endowment of stimuli-sensitivity for precise targeting of the cancer site. In this review, we summarize the recent efforts in developing novel targeting approaches via active endocytosis and stimuli-sensitive systems responding to hyperthermic or acidic tumor pH conditions.

Characterization of Chitin and Chitosan as a Biomedical Polymer (생체의료용 재료로써 키틴·키토산의 특성)

  • Jang, Mi-Kyeong;Nah, Jae-Woon
    • Applied Chemistry for Engineering
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    • v.19 no.5
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    • pp.457-465
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    • 2008
  • Development of various medical systems was accomplished through the progress of biotechnological method for therapy of human diseases. Furthermore, drug delivery systems have been investigated to carry the bioactive materials such as drug or gene in the body effectively. The most important thing in this system is to develop biomedical polymers having biocompatibility, biodegradability, and non-toxicity. Chitosan, a natural polymer, has been importantly considered as biomedical materials due to its good biocompatibility and various bio-active characteristics. Since the property of chitosan is differently explained according to the crystalline structures of chitin, the study for structural analysis of chitin has to proceed to apply as a biomaterial. From this point of view, this article introduced the analysis of crystalline structural of chitin, general property of chitosan and potential characteristics of low molecular weight water-soluble chitosan (LMWSC) as a biomaterials. Furthermore, chemical modification of LMWSC using various functional groups was also performed to enhance its bioavailability and emphasize their potential as drug delivery carriers (DDS).