Preparation of multicomponent nanoparticles for effective anti-inflammatory therapy
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Date
2020-08-23
Authors
Zohud, Nihal Ziad
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Publisher
An-Najah National University
Abstract
Background: Non-steroidal anti-inflammatory drugs are amongst the major common and widely prescribed drugs for pain and inflammation. However, their notoriety of causing gastrointestinal effects, their low water solubilities and their short half-lives would affect the patient compliance and the oral absorption of them and accordingly justify the need to have NSAIDs with controlled and sustained release manner in combination with anti-ulcer drugs. Recently, nanoparticles technology is considered an ingenious technique to overcome these drawbacks. Herein, we developed multi-drug delivery nanosystems of Indomethacin, Paracetamol and Famotidine using nanoemulsion and polymeric nanoparticles techniques.
Methodology: Starting from the synthesis of the Co-drug of Indomethacin and Paracetamol joined through a hydrolysable ester followed by pre-loading this Co-drug into nanoemulsion (Co-NE) which would be loaded into different polymeric nanoparticles having Famotidine utilizing nanoprecipitation approach. The developed nanosystems were characterized by transmission electron microscopy, dynamic light scattering and zeta potential analysis. Moreover, stability and biocompatibility studies were tested. In addition, a novel RP-HPLC method was developed and validated according to ICH guidelines to study the in vitro release profiles of the loaded drugs (FAM and Co-drug).
Results: These developed nanosystems showed a hydrodynamic size between 190-240 nm and the zeta potential values ranges from -30 to -48 mV. TEM images confirmed Co-NE loading into different polymeric nanoparticles. Stability studies revealed that these nanosystems were stable at different temperatures and buffered conditions over one month. Moreover, improvement of the solubilities of these three drugs using this encapsulation technique leading to have controlled-release multi component systems of both Co-drug and Famotidine over three days. In addition to quantification of the four drugs on one HPLC run by developing and validating a RP-HPLC method that was successfully utilized for quantification of the in vitro hydrolysis, release, loading and conversion of Co-drug.
Conclusion: These multi component nanoparticles might be a potential platform to overcome the obstacles of NSAIDs, synergize drugs with different mechanism of actions by co-encapsulating a small-sized nanoemulsion into different polymeric nanocarriers for reaching the goal of effective anti-inflammatory therapy.
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Keywords
anti-inflammatory therapy , multicomponent nanoparticles