“…Similarly, Tao et al. [ 96 ] presented a unique strategy using a polymer (poly (Pt (IV) prodrug)) bearing numerous carboxyl side groups and incorporating redox-sensitive cisplatin Pt (IV) prodrugs in its backbone as the payload for encapsulation in CPNPs ( Fig. 13 B).…”
Section: Application Of Calcium Phosphate Nanocarriersmentioning
confidence: 99%
“… Fig. 13 The CaP shell nanoparticles with different organic core: A) PEG-PBO [ 95 ], B) PEG-PAA [ 96 ], C) Curcumin/NaCas [ 99 ] and hyaluronic acid/Zn(II)-DPA [ 100 ], respectively. …”
Section: Application Of Calcium Phosphate Nanocarriersmentioning
“…Similarly, Tao et al. [ 96 ] presented a unique strategy using a polymer (poly (Pt (IV) prodrug)) bearing numerous carboxyl side groups and incorporating redox-sensitive cisplatin Pt (IV) prodrugs in its backbone as the payload for encapsulation in CPNPs ( Fig. 13 B).…”
Section: Application Of Calcium Phosphate Nanocarriersmentioning
confidence: 99%
“… Fig. 13 The CaP shell nanoparticles with different organic core: A) PEG-PBO [ 95 ], B) PEG-PAA [ 96 ], C) Curcumin/NaCas [ 99 ] and hyaluronic acid/Zn(II)-DPA [ 100 ], respectively. …”
Section: Application Of Calcium Phosphate Nanocarriersmentioning
“…10,11 To mitigate cisplatin's side effects, researchers have modified cisplatin ligands and altered different leaving groups, leading to the development of new divalent platinum drugs such as carboplatin, oxaliplatin, nedaplatin, and picoplatin, 12,13 as well as the design of Pt(IV) prodrug complexes with two axial ligands. [14][15][16][17] These platinum drug derivatives have to some extent reduced cisplatin's side effects but still cannot avoid certain drawbacks associated with small-molecule drugs, such as poor water solubility, ineffective accumulation at tumor sites, and low bioavailability. With the recent development of "polymeric nanomedicine" in recent years, 18,19 there is potential to provide technical avenues for overcoming this challenge.…”
A co-delivery system employing cisplatin and novel conjugated polymers is utilized to achieve synergistic chemotherapy/photothermal therapy for cancer treatment at lower drug concentrations.
“…In medicinal science, increasing the solubility of active pharmaceutical ingredients (APIs) to improve their bioavailability is a core objective. Several methods have been established to address this concern, including the use of prodrugs [ 1 , 2 , 3 , 4 , 5 ], nanosuspensions, [ 6 , 7 , 8 , 9 ] or complexation of APIs [ 10 , 11 , 12 , 13 , 14 ], and modification of the solid API phase itself. The latter approach can be achieved through the formation of API salts, co-crystals, or amorphous systems to enhance the targeted drug’s solubility properties [ 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 ].…”
In this study, we compare the mechanochemical and classical solvent crystallization methods for forming maleates of GABA and its pharmaceutically active derivatives: Pregabalin, Gabapentin, Phenibut, and Baclofen. Common characterization techniques, like powder and single crystal X-ray diffraction, IR-spectroscopy, differential scanning calorimetry, thermogravimetric analysis and 1H-NMR spectroscopy, are used for the evaluation of structural and physicochemical properties. Our work shows that maleate formation is possible with all investigated target compounds. Large increases in solubility can be achieved, especially for Pregabalin, where up to twentyfold higher solubility in its maleate compared to the pure form can be reached. We furthermore compare the mechanochemical and solvent crystallization regarding quickness, reliability of phase production, and overall product quality. A synthetic route is shown to have an impact on certain properties such as melting point or solubility of the same obtained products, e.g., for Gabapentin and Pregabalin, or lead to the formation of hydrates vs. anhydrous forms. For the GABA and Baclofen maleates, the method of crystallization is not important, and similarly, good results can be obtained by either route. In contrast, Phenibut maleate cannot be obtained pure and single-phase by either method. Our work aims to elucidate promising candidates for the multicomponent crystal formation of blockbuster GABA pharmaceuticals and highlight the usefulness of mechanochemical production routes.
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