Development and Preliminary Characterization of Polyester-Urethane Microparticles Used in Curcumin Drug Delivery System for Oropharyngeal Cancer

Abstract

Background and Objectives: Curcumin (Cc) as an active substance is known for its anti-inflammatory, anticoagulant, antioxidant, and anti-carcinogenic effects, together with its role in cholesterol regulation, and its use in different gastrointestinal derangements. On the other hand, curcumin can be used for its properties as an inactive substance, with Cc particles being more often tested in pharmaceutical formulations for drug delivery, with promising safety records and kinetics. The aim of this research was to obtain and characterize polyurethane microparticles that can be used as a carrier with a controlled Cc release. Materials and Methods: The in vitro samples were characterized by the Zetasizer procedure, and UV–Vis spectroscopy, while the in-vivo measurements on human subjects were performed by non-invasive skin assays (trans-epidermal water loss, erythema, and skin hydration). A total of 16 patients with oropharyngeal cancer stages II and III in equal proportions were recruited for participation. Results: The experimental values of sample characteristics using the Zetasizer identified a mean structural size of 215 nm in the polyester-urethane preparate (PU), compared to 271 nm in the curcumin-based PU. Although the size was statistically significantly different, the IPDI and Zeta potential did not differ significantly (22.91 mV vs. 23.74 mV). The average age during the study period was 57.6 years for patients in the PU group, respectively, and 55.1 years in those who received the curcumin preparations. The majority of oropharyngeal cancers were of HPV-related etiology. There were no significant side effects; 75.0% of patients in the PU group reporting no side effects, compared to 87.5% in the Cc group. The 48 h TEWL measurement at the end of the experiment found a statistically significant difference between the PU and the Cc group (2.2 g/h/m2 vs. 2.6 g/h/m2). The erythema assessment showed a starting measurement point for both research groups with a 5.1-unit difference. After 48 h, the difference between PU and PU_Cc was just 1.7 units (p-value = 0.576). The overall difference compared to the reference group with sodium lauryl sulfate (SLS) was statistically significant at a 95% significance level. Conclusions: Our findings indicate the obtaining of almost homogeneous particles with a medium tendency to form agglomerations, with a good capacity of encapsulation (around 60%), a medium release rate, and a non-irritative potential. Therefore, this polyester-urethane with Cc microparticles can be tested in other clinical evaluations.

The Influence of an Isocyanate Structure on a Polyurethane Delivery System for 2′-Deoxycytidine-5′-monophosphate

“…Despite the slight increase in erythema and decrease in skin hydration during assessment, the results obtained in this study indicate that the synthesized products do not alter the epidermal function with regard to the strong correlation between two skin parameters. A. Chioreanu et al describe a similar drug delivery system based on polyester-urethane microparticles used for curcumin, and they report similar differences in skin parameters between the samples and reference (sodium lauryl sulfate) [81].…”

Synthesis and Assessment of a Polyurethane Carrier Used for the Transmembrane Transfer of 2'-Deoxycytidine-5'-monophosphate sodium salt

“…Despite the slight increase of erythema and decrease of skin hydration during assessment, the results obtained in this study indicate that the synthesized products not alter the epidermal function, respectively the strong correlation between two skin parameters. A. Chireanu et al describe a similar drug delivery system based on polyester-urethane microparticles used for curcumin and they report similar differences of skin parameters between the samples and reference (sodium lauryl sulfate) [55].…”

Curcumin/Carrier Coprecipitation by Supercritical Antisolvent Route

“…Although it is a natural compound and therefore has less toxicity when compared with other active principle ingredients (APIs), this compound must often be administered at high concentrations due to its poor bioavailability, resulting from a low solubility in water [ 14 , 15 ]. To avoid the administration of considerable amounts of the API, it is often proposed as micronized powders [ 16 , 17 ]; moreover, to protect it from light and oxygen, it is often coprecipitated with a hydrophilic carrier [ 18 , 19 ]. Among the innovative techniques used in the pharmaceutical field to obtain carrier/active principle composites, the ones based on supercritical carbon dioxide (scCO 2 ) are particularly attractive [ 20 , 21 , 22 ].…”