This work aims to develop and optimize blended polylactide-co-glycolide (PLGA) and poly(ε-caprolactone, PCL) loaded with Boswellia sacra oil (BO) to improve BO’s physicochemical properties and anti-breast cancer effects via enhancing apoptosis. In this context, BO was extracted from B. sacra oleo gum resins (BO) via hydrodistillation and chemically characterized by evaluating its essential oil’s composition using gas chromatography–mass spectrometry. Then, BO/PLGA–PCL NPs were formulated using the emulsion (O/W) solvent evaporation technique using a PLGA–PCL mixture at five different ratios (1:1, 2:1, 3:1, 1:2, and 1:3, respectively). The optimized NPs had a spherical morphology with no agglomerations and the lowest hydrodynamic size (230.3 ± 3.7 nm) and polydispersity index (0.13 ± 0.03) and the highest ζ potential (−20.36 ± 4.89 mV), as compared to the rest of the formulas. PLGA–PCL NPs could entrap 80.59 ± 3.37% of the BO and exhibited a controlled, sustained release of BO (83.74 ± 3.34%) over 72 h. Encapsulating BO in the form of BO/PLGA–PCL NPs resulted in a lower IC50 value as assessed by the MTT assay. Furthermore and upon assessing the apoptotic effect of both BO and BO/PLGA–PCL NPs, there was an increase in the percentage of apoptotic and necrotic cell percentages compared to the control and free BO. Encapsulation of BO in PLGA–PCL NPs doubled the percentage of apoptotic and necrotic cells exerted by free BO. These findings support the potential use of BO/PLGA–PCL NPs in treating breast cancer.

No abstract

Ozonated olive oil (OL) combines the therapeutic effects of both ozone and olive oil. However, it suffers from limited water solubility and poor transdermal permeation, which hinder its application in melanoma treatment. Nanocarrier host molecules, such as niosomes, were used to improve the water solubility, transdermal permeation, and anticancer effect of hydrophobic compounds. This study aims to design and optimize a niosomal vesicular nanoplatform loaded with OL (OL/NSs) to improve OL’s skin permeation and anti-melanoma effect. In this regard, OL was prepared and characterized by evaluating its chemical properties (acid, peroxide, and iodine values) and fatty acid composition using gas chromatography. Then, OL/NSs were developed using the thin film hydration method employing cholesterol, Span 60, and Tween 60 at five different molar ratios. The optimized niosomes had an average diameter of 125.34 ± 13.29 nm, a surface charge of −11.34 ± 4.71 mV, and a spherical shape. They could entrap 87.30 ± 4.95% of the OL. OL/NSs showed a 75% sustained oil release over 24 h. The skin permeation percentage of OL/NSs was 36.78 ± 3.31 and 53.44 ± 6.41% at 12 and 24 h, respectively, three times higher than that of the free OL (11.50 ± 1.3 and 17.24 ± 2.06%, at 12 and 24 h, respectively). Additionally, the anticancer activity of the developed niosmal formulation, when tested on human melanoma cells (A375), was double that of the free OL; the IC50 of the OL/NSs was 8.63 ± 2.8 μg/mL, and that of the free OL was 17.4 ± 3.7 μg/mL. In conclusion, the encapsulation of ozonated olive oil in niosomes enhanced its water solubility, skin permeation, and anticancer activity and thus may represent potent natural chemotherapy in treating melanoma.

pH-responsive dual-loaded nanoplatforms based on polyamidoamine dendrimer with a hydroxyl-terminated surface (PAMAM–OH), generations 3, 4, and 5 (G3, G4, and G5, respectively), were loaded with Peganum harmala alkaloid extracts (H) and tannic acid (TA) and tested against breast cancer cells. G3 dendrimers encapsulating the drugs showed the smallest sizes, PDI, and highest ζ-potential and entrapment efficiencies compared to those of G4 and G5. G3 dendrimers loaded with either doxorubicin (DOX), H, or TA or dual-loaded with H+TA were prepared. The average diameters of the designed DOX@G3, H@G3, TA@G3, and H+TA@G3 NPs were 78 ± 5.1, 122 ± 3.7, 141 ± 2.8, and 192 ± 1.9 nm, respectively. All of the prepared NPs exhibited high positive surface charges and high entrapment efficiencies. Release studies showed the ability of the dendrimers to release their cargo selectively in the cancerous cells’ extracellular pH (pH 5.5) via a pH-triggered mechanism while maintaining an outstanding stability at physiological conditions (pH 7.4). Furthermore, H@G3, TA@G3, and H+TA@G3 NPs exhibited remarkable cytotoxic activities against breast adenocarcinoma (MCF-7) cells with IC50 values of 2.6 ± 0.08, 4.5 ± 0.9, and 1.7 ± 0.6 μg/mL, respectively, as compared to free H, free TA, free DOX, and DOX@G3 (IC50 values of 5.8 ± 0.8, 7.2 ± 1, 6.75 ± 0.7, and 4.7 ± 0.8 μg/mL). The formulated H@G3, TA@G3, and DOX@G3 exhibited 11.8, 9.3, and 5.3% increases in late apoptosis in MCF-7 cells relative to their respective free forms, while H+TA@G3 exhibited the highest percentage of late apoptosis in MCF-7 cells. In conclusion, G3 PAMAM–OH dendrimers dually loaded with Peganum harmala alkaloids and tannic acid hold the potential for effective treatment of breast cancer.

No abstract

No abstract