- Title
- Conjugation of isoniazid to a zinc phthalocyanine via hydrazone linkage for pH-dependent liposomal controlled release
- Creator
- Nkanga, Christian
- Creator
- Krause, Rui W M
- Subject
- To be catalogued
- Date Issued
- 2018
- Date
- 2018
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/194992
- Identifier
- vital:45517
- Identifier
- xlink:href="https://doi.org/10.1007/s13204-018-0776-y"
- Description
- Tuberculosis (TB) remains the leading cause of mortality from infectious diseases. Extended TB treatment and frequent adverse effects, due to poor bioavailability of anti-tubercular drugs (ATBDs), represent the main rationales behind liposomal encapsulation for controlled delivery. Liposomes have been reported as potential vehicles for targeted delivery of ATBDs due to their rapid uptake by macrophages, which are known as the main host cells for TB causative agent (Mycobacterium tuberculosis). Additionally, the need for controlled release of ATBDs arises because leakage is part of the key liposome challenges for hydrophilic compounds like isoniazid (INH). In this study, INH was conjugated to a highly hydrophobic photosensitizer, zinc (II) phthalocyanine (PC), through hydrazone bonding. The obtained conjugate (PC–INH) was encapsulated in liposomes by film hydration method. PC–INH loaded liposomes (PILs) were characterized using dynamic light scattering, transmission electron microscopy, energy-dispersive X-ray spectrometry and UV–Vis absorption spectrometry, which was used also for estimation of encapsulation efficiency (%EE). INH release was evaluated in different pH media using dialysis. Particle size, zeta potential and %EE of PILs were about 506 nm, − 55 mV and 72%, respectively. Over 12 h, PILs exhibited 22, 41, 97 and 100% of INH, respectively, released in pH 7.4, 6.4, 5.4 and 4.4 media. This pH-dependent behavior is attractive for site-specific delivery. These findings suggest the conjugation of chemotherapeutics to phthalocyanines using pH-labile linkages as a potential strategy for liposomal controlled release.
- Format
- computer
- Format
- online resource
- Format
- application/pdf
- Format
- 1 online resource (11 pages)
- Format
- Publisher
- SpringerNature
- Language
- English
- Relation
- Applied Nanoscience
- Relation
- Nkanga, C.I. and Krause, R.W.M., 2018. Conjugation of isoniazid to a zinc phthalocyanine via hydrazone linkage for pH-dependent liposomal controlled release. Applied Nanoscience, 8(6), pp.1313-1323
- Relation
- Applied Nanoscience volume 8 number 6 p. 1313 2018 1313–1323
- Rights
- Publisher
- Rights
- Use of this resource is governed by the terms and conditions of the SpringerNature Statement (https://www.biomedcentral.com/)
- Rights
- Open Access
- Hits: 798
- Visitors: 910
- Downloads: 119
Collections
Krause, Rui Werner Maçedo (Prof)
RU Department of Chemistry
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | Conjugation of isoniazid to a zinc phthalocyanine via hydrazone.pdf | 1 MB | Adobe Acrobat PDF | View Details Download |