Tracking of crystalline-amorphous transition of carvedilol in rotary spun microfibers and their formulation to orodispersible tablets for in vitro dissolution enhancement

Abstract

Physicochemical characterization of microfibers including powder X-ray diffraction, differential scanning calorimetry, attenuated total reflectance Fourier transform infrared spectroscopy, and positron annihilation spectroscopy were used to track the crystalline-amorphous transition of carvedilol during formulation and stability testing. The applied methods unanimously indicated the amorphous transition of carvedilol in the course of rotary spinning, furthermore a supramolecular ordering of chains of polymer matrix was revealed out by positron annihilation spectroscopy. The accelerated stability study (40±2°C/75±5% RH, for 4 weeks) indicated a large stress tolerance capacity of fibers, since only a partial crystallization of the active compound was observable at the last sampling point. To demonstrate possible utilization of microfibers, orodispersible tablets containing 10mg of carvedilol were successfully prepared by direct compression applying common tableting excipients. All of the investigated tablet parameters (hardness, friability, in vitro disintegration time) complied with the pharmacopoeial requirements. The performed dissolution (pH 1.0 and 6.8) study indicated that the drug dissolution from the microfiber based formula was rapid, complete and independent from the pH of the applied media, while the dissolution from the control tablets, containing crystalline carvedilol was incomplete and was strongly influenced by the pH of the applied media.

Recent applications of electrical, centrifugal, and pressurised emerging technologies for fibrous structure engineering in drug delivery, regenerative medicine and theranostics

“…Centrifugal spinning also been used to fabricate microfibers which were subsequently compressed into orodispersible tablets [394]. The dissolution of poorly water-soluble drug carvedilol was significantly enhanced compared to tablets comprising physical mixture of hydroxypropyl cellulose and raw drug.…”

Fiber Based Approaches as Medicine Delivery Systems

“…133 In rotary spinning, the fiber morphology is primarily controlled by adjusting the rotary speed, polymeric solution composition, and inner diameter of the wall orifices. 135 Szabo et al…”

“…In rotary spinning, the fiber morphology is primarily controlled by adjusting the rotary speed, polymeric solution composition, and inner diameter of the wall orifices. 135 Szabo et al fabricated hydroxypropyl cellulose fibers by rotary spinning, which were subjected to a preformulation study. This is a stage in drug development where the morphological and chemical properties of a therapeutic substance are characterized.…”

“…The material composition and function are given. 135 Hydroxypropyl cellulose Semisynthetic alkaloid N/A 12.6 ± 4.8 μm to 13.5 ± 6.1 μm Promoting neurite outgrowth and inhibit glial differentiation Tysseling-Mattiace et al 149 IKVAV PA regeneration of both sensory and motor neurons, reduction in cell mortality Guo et al 150 RADA16-I peptide Reknitting the injured spinal cord Shah et al 140 TGFBPA cartilage regeneration Davis et al 141 RAD16-II peptide Promote vascular cell recruitment in the myocardium. Stendahl et al 142 Heparin-binding peptide amphiphiles Improvement in pancreatic islet engraftment Schneider et al 145 self-complementary peptides with 16 amino-acids (RADA16-I, Ac-RADARADARADARADA-CONH2) Acceleration of wound healing Galler et al 146 13-amino-acid peptide (GTAGLIGQERGDS) Dental carrie replacement with dental stem cells Brun et al 147 Several peptides with varying sequences.…”

Improved Dissolution Rate of Oxcarbazepine by Centrifugal Spinning: In-Vitro and In-Vivo Implications

“…Majority of newly developed active pharmaceutical ingredient (APIs) are poorly soluble owing to their lipophilic nature [1]. This leads to low dissolution rate and in turn poor bioavailability of these drugs [2]. Majority of these drugs belongs to BCS class II [3].…”