کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10229673 | 546 | 2011 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
pH-responsive endosomolytic pseudo-peptides for drug delivery to multicellular spheroids tumour models
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
مهندسی شیمی
بیو مهندسی (مهندسی زیستی)
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: pH-responsive endosomolytic pseudo-peptides for drug delivery to multicellular spheroids tumour models pH-responsive endosomolytic pseudo-peptides for drug delivery to multicellular spheroids tumour models](/preview/png/10229673.png)
چکیده انگلیسی
Endosomolytic polymers can aid in the endosomal release of therapeutics to improve intracellular drug delivery. pH-responsive biomimetic pseudo-peptides were synthesised by grafting l-phenylalanine onto the pendant carboxylic acids of a polyamide, poly(l-lysine isophthalamide). PP-75 (stoichiometric l-phenylalanine grafting of 75Â mol%) was determined to have the best endosomolytic property. The mean hydrodynamic size of PP-75 decreased with lower pH as the polymers adopted a more compact conformation due to protonation of acidic groups and increase in hydrophobicity. PP-75 was demonstrated to deliver model drugs effectively in three dimensional (3D) magnetic HeLa multicellular spheroids used as in vitro tumour models. These spheroids can be isolated easily and quickly by magnetic separation. Due to its relatively small size, PP-75 was able to penetrate from the exterior to the interior of these spheroids and was internalised by the cells in the spheroids. It could retain its pH-mediated membrane-lytic capability in 3D drug delivery by releasing internalised calcein from intracellular endosomes in the tumour models. Furthermore, cell viability results suggest that PP-75 showed no significant cytotoxicity towards cells in the spheroids. The pH-responsive PP-75 can potentially enhance the extracellular and intracellular delivery of therapeutics in tumours.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biomaterials - Volume 32, Issue 11, April 2011, Pages 2953-2958
Journal: Biomaterials - Volume 32, Issue 11, April 2011, Pages 2953-2958
نویسندگان
Vincent H.B. Ho, Nigel K.H. Slater, Rongjun Chen,