Gum-based nanocapsules comprising naphthoquinones enhance the apoptotic and trypanocidal activity against Trypanosoma evansi

Nanoencapsulation is a promising approach to enhance the therapeutic potential of a drug. Herein, three selected naphthoquinone (NTQ) derivatives, based on the IC₅₀ value against Trypanosoma evansi, were encapsulated using gum damar as biocompatible and biodegradable natural gum via nanoprecipitation method. Nanoformulation of NTQs (NNTQs) was less than 150 nm in size, was found to be stable and released the drug in a sustained manner.

Highlights

Gum-based-naphthoquinone-loaded nanocapsules (NNTQs) are prepared via nanoprecipitation method.

NNTOs are evaluated against a parasite, Trypanosoma evansi, a causative agent for animal trypanosomosis.

NNTQs exhibit better antitrypanosomal effect at ∼1.5–4.0 times lesser doses as compared to native NTQs.

NNTQs improve production of reactive oxygen species and enhances apoptotic-like effect relative to NTQs against T. evansi.

All the three NNTQs exhibited significant antitrypanosomal effect and morphological changes at approximately two to three times lesser drug concentrations. The nanoformulations exhibited enhanced production of reactive oxygen species (ROS) in the axenic culture of T. evansi and less cytotoxic effect on horse peripheral blood mononuclear cells relative to pure NTQs.

As evidenced by flow cytometry, the NNTQs showed dose-dependent and time-dependent increased transition of live cells (AV^–PI^–) to early apoptotic cells (AV⁺PI⁻), late apoptotic cells (AV⁻PI⁺), and necrotic cells (AV⁺PI⁺) using annexin V/propidium iodide probe analysis. The results concluded that NNTQs induced more ROS, apoptosis and necrotic effects that exhibited more inhibitory effect on the growth of T. evansi with respect to respective NTQ by themselves.

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Article information: Ruma Rani, Balasubramanian Narsiman, Rajender S. Varma, Rajender Kumar,
Gum-based nanocapsules comprising naphthoquinones enhance the apoptotic and trypanocidal activity against Trypanosoma evansi, European Journal of Pharmaceutical Sciences, Volume 171, 2022. https://doi.org/10.1016/j.ejps.2022.106118.