Taste Masking of Promethazine Hydrochloride Using l-Arginine Polyamide-Based Nanocapsules

Abstract

Promethazine hydrochloride (PMZ), a potent H1-histamine blocker widely used to prevent motion sickness, dizziness, nausea, and vomiting, has a bitter taste. In the present study, taste masked PMZ nanocapsules (NCs) were prepared using an interfacial polycondensation technique. A one-step approach was used to expedite the synthesis of NCs made from a biocompatible and biodegradable polyamide based on l -arginine. The produced NCs had an average particle size of 193.63 ± 39.1 nm and a zeta potential of −31.7 ± 1.25 mV, indicating their stability. The NCs were characterized using differential scanning calorimetric analysis and X-ray diffraction, as well as transmission electron microscopy that demonstrated the formation of the NCs and the incorporation of PMZ within the polymer. The in vitro release study of the PMZ-loaded NCs displayed a 0.91 ± 0.02% release of PMZ after 10 min using artificial saliva as the dissolution media, indicating excellent taste masked particles. The in vivo study using mice revealed that the amount of fluid consumed by the PMZ-NCs group was significantly higher than that consumed by the free PMZ group (p < 0.05). This study confirmed that NCs using polyamides based on l -arginine and interfacial polycondensation can serve as a good platform for the effective taste masking of bitter actives.

Development and Characterization of Transdermal Patches Using Novel Thymoquinone-L-Arginine-Based Polyamide Nanocapsules for Potential Use in the Management of Psoriasis

“…4d did not reveal any endothermic peak of TQ while the shallow peaks of the glass transition and evaporation are still present. It is proposed that TQ may have transformed into an amorphous material, hence an improved solubility, or the drug is encapsulated within the polymer as reported by other researchers [36,49].…”

“…These polymers have been used as carriers to facilitate insulin transdermal delivery, improve medication diffusion and distribution via the skin [35], and successfully deliver high doses of TQ into the lungs using dry powder inhalers [7]. Additionally, L-arginine-based polyamide was used to encapsulate promethazine HCl and produce taste-masked nanoparticles [36], while unsaturated L-arginine-poly(ester amide)s in an aqueous solution were used to create cationic hydrogels [37]. In recent studies, L-arginine-based polymers were found to be effective in gene transportation, gene condensation, and release [38].…”

Quality by Design for the Synthesis and Optimisation of Arginine-Poly(Ester-Amide) Nanocapsules as Promising Carriers for Nose-Brain Delivery of Carbamazepine

“…The other phase consists of terephthaloyl chloride and CBZ in chloroform (CHCl 3 ). Using this method, direct encapsulation of CBZ resulted in capsules with an average diameter around 400 nm and high-efficiency drug loading of 19.8% [52].…”