Abstract
Drug–drug cocrystals are formulated to produce combined medication, not just to modulate active pharmaceutical ingredient (API) properties. Nano-crystals adjust the pharmacokinetic properties and enhance the dissolution of APIs. Nano-cocrystals seem to enhance API properties by combining the benefits of both technologies. Despite the promising opportunities of nano-sized cocrystals, the research at the interface of nano-technology and cocrystals has, however, been described to be in its infancy. In this study, high-pressure homogenization (HPH) and high-power ultrasound were used to prepare nano-sized cocrystals of 4-aminosalysilic acid and sulfamethazine in order to establish differences between the two methods in terms of cocrystal size, morphology, polymorphic form, and dissolution rate enhancement. It was found that both methods resulted in the formation of form I cocrystals with a high degree of crystallinity. HPH yielded nano-sized cocrystals, while those prepared by high-power ultrasound were in the micro-size range. Furthermore, HPH produced smaller-size cocrystals with a narrow size distribution when a higher pressure was used. Cocrystals appeared to be needle-like when prepared by HPH compared to those prepared by high-power ultrasound, which had a different morphology. The highest dissolution enhancement was observed in cocrystals prepared by HPH; however, both micro- and nano-sized cocrystals enhanced the dissolution of sulfamethazine.
Highlights
Pharmaceutical cocrystals have been utilized to enhance the solubility and bioavailability [1], among other physicochemical properties, of active pharmaceutical ingredients (APIs)
Cocrystals prepared by high-pressure homogenization (HPH) were needle-shaped, as observed by TEM (Figure 2a–c)
Cocrystals prepared by high-power ultrasound sound had comparable crystallinity regardless of amplitude and time, ranging had comparable crystallinity regardless of amplitude and time, ranging fromfrom
Summary
Pharmaceutical cocrystals have been utilized to enhance the solubility and bioavailability [1], among other physicochemical properties, of active pharmaceutical ingredients (APIs). Patients failing to respond to multiple first-line TB medications have to use expensive second-line TB drugs, which include aminoglycosides, polypeptides, fluoroquinolones, thioamides, cycloserine, and 4-aminosalicylic acid (4-ASA) [16] Many of these antibiotics were developed decades ago and suffer from toxic side effects, administration difficulty, and poor activity against Mycobacterium tuberculosis [6]. Despite the promising opportunities of nano-sized cocrystals, research at the interface of nano-technology and cocrystals has been described to be in its infancy [35,45] In this regard, our aim in this study was to prepare and characterize nano-sized multi-drug cocrystals and to establish the effect of homogenization and high-power ultrasound parameters on size distribution, dissolution rate, thermal stability, degree of crystallinity, and polymorphic form produced. For the purpose of examining the effect of the method parameters, different pressures were used to perform HPH, operating with different cycle runs, while high-power ultrasound cocrystallization was carried out using different amplitudes and different process durations
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