Pharmacokinetic study of an oral piroxicam formulation containing different molar ratios of β-cyclodextrins

Sarakha, Mohamed; Bouchal, Fatiha; Boukhris, T.; Bounoure, F.; Fessi, Hatem; Fatmi, Sofiane; Chaffai, N.; Lahiani-Skiba, Malika

doi:10.1007/s10847-012-0166-0

Cited by 10 publications

(4 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Isotretinoin (13-cis retinoic acid) [58] 25 (HPβCD susp., D:CD mole ratio 1:50) 1.00 [59] 10 (βCD susp., D:CD mole ratio 1:1) Humans HPβCD soln., D:CD mole ratio 1:2) -1.80 - [61] a Predicted data from ACS [45] b Based on reported phase-solubility studies if detailed descriptions are missing. c Relative bioavailability where the formulation containing no cyclodextrin is the reference formulation.…”

Section: 9mentioning

confidence: 99%

Pharmacokinetics of cyclodextrins and drugs after oral and parenteral administration of drug/cyclodextrin complexes

Loftsson

Moya‐Ortega

Alvarez‐Lorenzo

2015

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

Objectives The objective of the present study was to shed some light on pharmacokinetics of cyclodextrins (CDs) and drugs after oral and parenteral administration of inclusion complexes. Key findings The complex binding constant in water can predict pharmacokinetics after parenteral administration, but it has to be considered in the context of the physiological environment, where plasma proteins compete with CDs for drug binding. Neither drug/CD nor drug/protein complexes can extravasate, but differently from proteins, CDs are readily cleared through glomerular filtration. In such intricate interrelationships, for complexes with low-to-mid binding constant, binding of drug to plasma proteins will mainly dictate the pharmacokinetics. Oppositely, for drugs showing large CD complex binding constant and low protein binding, significant decrease in distribution volume and enhanced excretion of unmetabolized drug are observed; thus, relevant changes in bioavailability can be predicted. In the case of oral administration, volume for dilution/dissolution of the complexes is relatively low and hence excess CD can hamper drug absorption from the gastrointestinal (GI) tract. Summary CDs are well-established multipurpose excipients for overcoming organoleptic and biopharmaceutical deficiencies of a variety of drugs. Balances between free and complexed drug in the GI tract and between drug-CD binding and drug-protein binding in plasma seem to play a relevant role in drug pharmacokinetics.

show abstract

Section: 9mentioning

confidence: 99%

Pharmacokinetics of cyclodextrins and drugs after oral and parenteral administration of drug/cyclodextrin complexes

Loftsson

Moya‐Ortega

Alvarez‐Lorenzo

2015

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

show abstract

Section: Introductionmentioning

confidence: 99%

“…In this context, the use of pharmaceutical excipients, such as cyclodextrin (CD) for poorly soluble drugs (herein Px), can drastically boost its bioavailability without the requirement for a toxic solvent or a carrier polymer matrix. 12 The electrospinning technique offers great potential for the development of nanofibrous oral drug carriers. In this regard, electrospun nanofibers could be produced using a single fluid, 13,14 coaxial, 15 triaxial, 16 and other complex processes.…”

Section: Introductionmentioning

confidence: 99%

“…Due to Px’s poor solubility in water, it can be dissolved using organic solvents, surfactants, or acids to boost its loading content in the drug delivery systems. , However, this might cause adverse health effects on the oral administration of the Px drug over solvent traces. In this context, the use of pharmaceutical excipients, such as cyclodextrin (CD) for poorly soluble drugs (herein Px), can drastically boost its bioavailability without the requirement for a toxic solvent or a carrier polymer matrix …”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Rapid Sublingual Delivery of Piroxicam from Electrospun Cyclodextrin Inclusion Complex Nanofibers

Topuz

2022

ACS Omega

View full text Add to dashboard Cite

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.

show abstract

Industrial Applications of Cyclodextrins

Wang¹

2019

Handbook of Macrocyclic Supramolecular Assembly

View full text Add to dashboard Cite

Pharmacokinetic study of an oral piroxicam formulation containing different molar ratios of β-cyclodextrins

Cited by 10 publications

References 22 publications

Pharmacokinetics of cyclodextrins and drugs after oral and parenteral administration of drug/cyclodextrin complexes

Pharmacokinetics of cyclodextrins and drugs after oral and parenteral administration of drug/cyclodextrin complexes

Rapid Sublingual Delivery of Piroxicam from Electrospun Cyclodextrin Inclusion Complex Nanofibers

Industrial Applications of Cyclodextrins

Contact Info

Product

Resources

About