Abstract：
:We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 μm in length and ∼7 μm in diameter). SHS can physically disrupt skin in a dose-dependent manner and retain within the skin over at least 72 h, which allows sustained skin penetration of hydrophilic biomacromolecules. The magnitude of enhancement of FD delivery into skin induced by SHS treatment was dependent on its molecular weight. Specifically, SHS topical application enhanced FD-10 (MW: 10 kDa) penetration into porcine skin in vitro by 33.09 ± 7.16-fold compared to control group (p < 0.01). SHS dramatically increased the accumulation of FD-10 into and across the dermis by 62.32 ± 13.48-fold compared to the control group (p < 0.01). In vivo experiments performed using BALB/c mice also confirmed the effectiveness of SHS topical application; the skin absorption of FD-10 with SHS topical application was 72.14 ± 48.75-fold (p < 0.05) and 15.39 ± 9.91-fold (p < 0.05) higher than those from the PBS and Dermaroller microneedling, respectively. Further, skin irritation study and transepidermal water loss (TEWL) measurement using guinea pig skin in vivo indicated that skin disruption induced by SHS treatment is self-limited and can be recovered with time and efficiently. SHS can offer a safe, effective, and sustained skin delivery of hydrophilic biomacromolecules and presents a promising platform technology for a wide range of cosmetic and medical applications.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Zhang S,Ou H,Liu C,Zhang Y,Mitragotri S,Wang D,Chen Mdoi
10.1021/acs.molpharmaceut.7b00468subject
Has Abstractpub_date
2017-09-05 00:00:00pages
3188-3200issue
9eissn
1543-8384issn
1543-8392journal_volume
14pub_type
杂志文章abstract：:In the drug discovery setting, the ability to rapidly identify drug absorption risk in preclinical species at high doses from easily measured physical properties is desired. This is due to the large number of molecules being evaluated and their high attrition rate, which make resource-intensive in vitro and in silico ...
journal_title：Molecular pharmaceutics
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pub_type： 杂志文章
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pub_type： 杂志文章
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更新日期：2015-02-02 00:00:00
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doi：10.1021/mp050035b
更新日期：2005-11-01 00:00:00
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pub_type： 杂志文章
doi：10.1021/acs.molpharmaceut.7b01128
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更新日期：2019-09-03 00:00:00
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更新日期：2016-05-02 00:00:00
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journal_title：Molecular pharmaceutics
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更新日期：2018-09-04 00:00:00
