Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

Abstract

Chitosan is a valued excipient due to its biocompatibility properties and increasing solubility of poorly water-soluble drugs. The research presented in this paper concerns the preparation of binary combinations of chitosan (deacetylated chitin) with carvedilol (beta-blocker) to develop a formulation with a modified carvedilol release profile. As part of the research, six physical mixtures of chitosan with carvedilol were obtained and identified by spectral (PXRD, FT-IR, and Raman), thermal (DSC), and microscopic (SEM) methods. The next stage of the research estimated the profile changes and the dissolution rate for carvedilol in the obtained drug delivery systems; the reference sample was pure carvedilol. The studies were conducted at pH = 1.2 and 6.8, simulating the gastrointestinal tract conditions. Quantitative changes of carvedilol were determined using the developed isocratic UHPLC-DAD method. Established apparent permeability coefficients proved the changes in carvedilol’s permeability after introducing a drug delivery system through membranes simulating the gastrointestinal tract and skin walls. A bioadhesive potential of carvedilol–chitosan systems was confirmed using the in vitro model. The conducted research and the obtained results indicate a significant potential of using chitosan as an excipient in modern oral or epidermal drug delivery systems of carvedilol.

Intranasal Delivery of Carvedilol- and Quercetin-Encapsulated Cationic Nanoliposomes for Cardiovascular Targeting: Formulation and In Vitro and Ex Vivo Studies

“…For 3-[(2-methoxyphenoxyethyl) amino]-2-propanol moiety of CVD, the characteristic peaks observed at 1014 cm –1 (C–O stretching), 1065 cm –1 (C–C stretching), 1594 cm –1 (CC stretching), and 1241 cm –1 (C–O–H bending and C–H rocking vibrations). Similar Raman spectra of CVD were reported by Sip et al, where they reported shifts at 727 cm –1 for C–C–C bending vibration, 867 and 1225 cm –1 for N–H bending, 1048, 1103, 1155, 1225, and 1509 cm –1 for C–H bending, 1334 cm –1 for C–N–C bending, 1013, 1285, 1460, and 1490 cm –1 for C–C, 1065 cm –1 for C–O, and 1631 cm –1 for CC vibration in 1-(9H-carbazol-4-yloxy) moiety, whereas bands for 3-[2-(2-methoxyphenoxy)ethyl amino]propan-2-ol moiety of CVD showed C–O, C–C, and CC stretching and C–O–H bending and C–H rocking vibrations at 1013, 1065, 1591, and 1241 cm –1 . The broad Raman peaks of pure QC were observed at 1661 cm –1 (C 4 O 2 stretching), 1609 cm –1 (C 2 C 3 stretching and C 3 /C 5 –OH bending) of phenyl and benzo rings, 1592 cm –1 (CO stretching) and 1552 cm –1 (C–C stretching) of ring B.…”

Chitosan as a Functional Carrier for the Local Delivery Anti-Inflammatory Systems Containing Scutellariae baicalensis radix Extract

“…It can be used in pharmaceutical excipients or drug carriers [ 4 ], wound-healing materials [ 5 ], and as a scaffold for tissue engineering [ 6 ]. Chitosan is often used in pharmaceutical technology as an ingredient controlling and delaying the release of both synthetic [ 7 , 8 , 9 ] and natural ingredients [ 10 , 11 ].…”

Amorphous Form of Carvedilol Phosphate—The Case of Divergent Properties

“…The condition limiting the bioavailability of drugs belonging to the BCS II class, characterized by good permeability through biological membranes, is their low solubility in the water environment. Carvedilol belonging to this group of drugs shows solubility dependent on the pH of the environment; it dissolves much better in acidic conditions due to the transition to the ionic form, while it precipitates at the reduced pH of the intestine [ 46 ]. According to the USP guidelines, the test for carvedilol tablets is performed at acidic pH; however, the conducted tests indicate its highest absorption in the jejunum lumen [ 47 , 48 , 49 ].…”