Title:Ketorolac Tromethamine Loaded Nano-Spray Dried Nanoparticles: Preparation,
Characterization, Cell Viability, COL1A1 Gene Simulation and
Determination of Anti-inflammatory Activity by In vivo HET-CAM Assay
Volume: 20
Issue: 6
Author(s): A.A. Öztürk*, T. Çevikelli, E.K. Tilki, U.M. Güven and H.T. Kıyan
Affiliation:
- Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, Eskişehir, Türkiye
Keywords:
Ketorolac tromethamine, wound, HET-CAM, RT-PCR, COL1A1, nanoparticle, KT-NP.
Abstract:
Background: Ketorolac tromethamine (KT) is a non-steroidal anti-inflammatory drug from
the heteroaryl acetic acid derivatives family. The most widely used new nanotechnological approaches
for topical drug delivery are polymeric nanoparticles (NPs).
Objective: Successful results have been obtained with low doses in many treatments, such as cancer,
antimicrobial, pain, made with nanoparticle formulations of drug active ingredients.
Methods: NPs were prepared using Nano Spray-Dryer. The cytotoxicity of the optimum formulation in
BJ (ATCC® CRL-2522™) human fibroblast cells was determined by the WST- 1 method and the gene
activity was elucidated by mRNA isolation and real-time polymerase chain reaction (RT-PCR). The in
vivo HET- CAM assay was performed for anti-inflammatory activity.
Results: NPs presented PDI values lower than 0.5, and therefore particle size distribution was decided
to be monodisperse. Positive zeta potential values of NPs highlighted the presence of the cationic ammonium
group of Eudragit® RS 100. The release rates observed from KT-NP coded formulations after
24 hours were 78.4% ± 2.9, demonstrating extended release from all formulations, relative to pure KT.
The lowest concentration of KT-NP increased fibroblast cell proliferation higher than the highest concentration
of KT. The 5-fold increased effect of KT-NP formulation on collagen gene expression compared
to KT is also related to the enhanced anti-inflammatory effect in line with the in vivo HET-CAM
assay results.
Conclusion: With the obtained cell viability, gene expression, and HET-CAM results, it has the hope of
a successful nano-topical formulation, especially in both wound healing and anti-inflammatory treatment.
