Rapid Sublingual Delivery of Piroxicam from Electrospun Cyclodextrin Inclusion Complex Nanofibers

Abstract

Piroxicam (Px) is a nonsteroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis and rheumatoid arthritis. It is administered orally; however, its poor water solubility causes low loading to the nonconventional drug delivery systems (DDSs), such as electrospun fibers. Furthermore, the rapid dissolution of DDS and fast release of the embedded drugs are crucial for oral delivery of drugs to patients who are unconscious or suffering from dysphagia. In this regard, this study reports the development of rapidly dissolving cyclodextrin (CD)-based inclusion complex (IC) nanofibers by waterborne electrospinning for fast oral delivery of Px. Scanning electron microscopy analysis revealed the formation of bead-free fibers with a mean diameter range of 170–500 nm at various concentrations of Px; increasing the Px loading decreased the fiber diameter. The formation of IC was demonstrated by X-ray diffraction (XRD) analysis by the disappearance of crystalline peaks of Px. Likewise, differential scanning calorimetry (DSC) analysis showed the disappearance of the melting peak of the embedded Px due to IC formation. Both Fourier transform infrared (FTIR) and thermogravimetric analysis (TGA) confirmed the presence of Px within the fibers. 1 H NMR experiments demonstrated Px preservation in the fibers after six months. Px-loaded nanofibers were employed for sublingual drug delivery. To mimic the environment of the mouth, the nanofibers were treated with artificial saliva, which revealed the instant dissolution of the nanofibers. Furthermore, dissolution experiments were performed on the tissues wetted with artificial saliva, where the dissolution of the fibers could be extended to a few seconds, demonstrating the suitability of the materials for sublingual oral drug delivery. Overall, this paper, for the first time, reports the rapid oral delivery of Px from polymer-free CD fibers produced by waterborne electrospinning without the requirement of any carrier polymer and toxic solvent.

Nanoencapsulation of Menthol/Cyclodextrin Inclusion Complexes in Rapidly Dissolving Electrospun Gelatin Nanofibers

“…As revealed by XRD analysis, the fibers are amorphous and have a large surface-to-volume ratio, which accelerates the fiber dissolution. The rapid dissolution of CD ICs fibers − and gelatin fibers is generic . The dissolution time could be prolonged with the use of a hydrophobic polymer during the fabrication of electrospun fibers.…”

Cyclodextrin Inclusion Complexes for Improved Drug Bioavailability and Activity: Synthetic and Analytical Aspects

“…The production of nanofibers based on inclusion complexes with β-CD and polycaprolactone and gelatin as polymeric materials has enhanced drug release and pharmacological activity [ 99 ]. Significant improvements in the solubility of hydrocortisone [ 100 ] and piroxicam [ 101 ] have been reported due to the high degree of wetting of the nanofibers obtained via electrospinning from the inclusion complexes with HPβ-CD, with the advantage of not using additional polymeric materials.…”

Super porous α‐, β‐, γ‐cyclodextrin cryogels with high active agent loading and controllable release profiles

“…In the presence of water, the functional components encapsulated with CDs form "molecular dispersions" resulting in much better bioavailability of hydrophobic substances. 2,8 In addition, various physicochemical properties of the guest molecules properties such as solubility, 10 degradation, 11 and stability 12 can be improved significantly. The inclusion complexes of CDs with different molecules can be used in a variety of industries including the food industry, cosmetics, chemistry, agriculture, textile, and most importantly drug development [13][14][15] and biomedical industries.…”