- Title
- Inclusion complexation and liposomal encapsulation of an isoniazid hydrazone derivative in cyclodextrin for pH-dependent controlled release
- Creator
- Safari, Justin B, Mona, Lamine B, Sekaleli, Bafokeng T, Avudi, Bénite K, Isamura, Bienfait K, Mukubwa, Grady K, Salami, Sodeeq A, Mbinze, Jérémie K, Lobb, Kevin A, Krause, Rui W M, Nkanga, Christian I
- Subject
- To be catalogued
- Date
- 2023
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/452727
- Identifier
- vital:75166
- Identifier
- xlink:href="https://doi.org/10.1016/j.jddst.2023.104302"
- Description
- Tuberculosis, a predominantly pulmonary pathology, is currently the deadliest infection worldwide. Its treatment is based on combination therapy involving selected antimicrobials including Isoniazid. However, physicochemical properties of isoniazid negatively affect the clinical performance of current tuberculosis regimens, causing drug resistance development and increasing mortality rates. Liposomal encapsulation improves antituberculosis drug delivery; however, nano-formulation of isoniazid remains challenging due to its small molecular size and high hydrophilicity. Therefore, this study aimed to derivatize isoniazid and formulate a controlled delivery system using the concept of drug-in-cyclodextrins-in-liposomes to enhance drug biopharmaceutical properties. A prodrug of isoniazid was synthesized and screened for its ability to form stable complexes with α, β, and γ cyclodextrins. A selected inclusion complex with β-cyclodextrin was encapsulated in liposomes and assessed for controlled release of isoniazid. Successful formation of a 1:1 complex was established and characterized, followed by molecular modeling studies to demonstrate strength of the interactions within the complex and predicted complex structure. The inclusion complex was successfully encapsulated in liposomes using the thin film hydration method and the ethanol injection ultrasonic dispersion, with the latter giving the best results. These findings demonstrate the potential.
- Format
- computer, online resource, application/pdf, 1 online resource (12 pages), pdf
- Publisher
- Elsevier
- Language
- English
- Relation
- Journal of Drug Delivery Science and Technology, Safari, J.B., Mona, L.B., Sekaleli, B.T., Avudi, B.K.N., Isamura, B.K., Mukubwa, G.K., Salami, S.A., Mbinze, J.K., Lobb, K.A., Krause, R.W.M. and Nkanga, C.I., 2023. Inclusion complexation and liposomal encapsulation of an isoniazid hydrazone derivative in cyclodextrin for pH-dependent controlled release. Journal of Drug Delivery Science and Technology, 81, p.104302, Journal of Drug Delivery Science and Technology volume 81 p. 104302 2023 2588-8943
- Rights
- Publisher
- Rights
- Use of this resource is governed by the terms and conditions of the Elsevier Terms and Conditions Statement (https://www.elsevier.com/legal/elsevier-website-terms-and-conditions)
- Rights
- Closed Access
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- Visitors: 374
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Collections
Krause, Rui Werner Maçedo (Prof)
Lobb, Kevin Allan (Assoc Prof)
RU Department of Chemistry
SDG 03. Good Health and Well-Being
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details | SOURCE1 | Inclusion complexation and liposomal encapsulation of an isoniazid hydrazone derivative in cyclodextrin for pH-dependent controlled release.pdf | 823 KB | Adobe Acrobat PDF | View Details |