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Recent advances in anticoagulant drug delivery
Park, Jooho,Byun, Youngro Informa UK (Ashley Publications) 2016 Expert opinion on drug delivery Vol.13 No.3
<P>Introduction: Anticoagulants have been prescribed to patients to prevent deep vein thrombosis or pulmonary embolism. However, because of several problems in anticoagulant therapy, much attention has been directed at developing an ideal anticoagulant, and numerous attempts have been made to develop new anticoagulant delivery systems in recent years. Areas covered: This review discusses the challenges associated with the recent development of anticoagulants and their delivery systems. Various delivery methods have been developed to improve the use of anticoagulants. Recent advances in anticoagulant delivery and antidote development are also discussed in the context of their current progression states. Expert opinion: There have been many different approaches to developing the delivery system of anticoagulants. One approach has been to expand the use of new oral agents and develop their antidotes. Reducing the size of heparins to use smaller heparins for delivery, and developing oral or topical heparins are also some of the approaches used. Various physical formulations or chemical modifications are other ways that have enhanced the therapeutic potential of anticoagulant agents. On the whole, recent advances have contributed to increasing the efficacy and safety of anticoagulant clinically and have benefited the field of anticoagulant delivery.</P>
Jeon, Ok-Cheol,Byun, Youngro,Park, Jin Woo American Scientific Publishers 2016 Journal of Nanoscience and Nanotechnology Vol.16 No.2
<P>To prepare orally available oxaliplatin (OXA), nanocomplexes were formed by ionic conjugation of OXA with the deoxycholic acid derivative, N-alpha-deoxycholyl-L-lysyl-methylester (DCK), as an oral absorption enhancer. We characterized the DCK-conjugated OXA nanocomplexes by differential scanning calorimetry, particle size determination, and morphological analysis. To evaluate the effects of DCK on the intestinal permeability of OXA, we assessed the solubilities and partition coefficients of OXA and the OXA/DCK nanocomplex, and then conducted in vitro artificial intestinal membrane and Caco-2 cell permeability studies. Finally, bioavailability in rats and tumor growth inhibition in the squamous cell carcinoma (SCC7) model after oral administration of the OXA/DCK nanocomplex were investigated compared to pure OXA. Analysis of the ionic complex formation of OXA with DCK revealed that OXA existed in an amorphous form within the complex, resulting in formation of nanocomplexes (35.05 +/- 4.48 nm in diameter). The solubility of OXA in water was approximately 7.07 mg/mL, whereas the water solubility of OXA/DCK was approximately 2.04 mg/mL and its partition coefficient was approximately 1.2-fold higher than that of OXA. The in vitro intestinal membrane permeability of OXA was significantly enhanced by complex formation with DCK. An in vivo pharmacokinetic study revealed that the C-max value of the OXA/DCK nanocomplex was 3.18-fold higher than that of OXA (32.22 +/- 10.24 ng/mL), and the resulting oral bioavailability of the OXA/DCK nanocomplex was 39.3-fold more than that of OXA. Furthermore, the oral administration of OXA/DCK significantly inhibited tumor growth in SCC7-bearing mice, and maximally inhibited tumor volume by 54% compared to the control. These findings demonstrate the therapeutic potential of the OXA/DCK nanocomplex as an oral anti-cancer therapy because it improves the oral absorption of OXA, which may improve patient compliance and expand the therapeutic applications of OXA to the prevention of recurrence and metastasis.</P>