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Nanomedicines for Ocular NSAIDs: State-of-the-Art Update of the Safety on Drug Delivery
Published in Lajos P. Balogh, Nano-Enabled Medical Applications, 2020
Joana R. Campos, Joana Araújo, Elisabet Gonzalez-Mira, Maria A. Egea, Elena Sanchez-Lopez, Marta Espina, Selma B. Souto, Maria L. Garcia, Eliana B. Souto
Chitosan was the most studied polymer, with a number of reports that claim its low toxicity and good biocompatibility following topical administration to rabbits and also cell cultures [68, 79, 110, 225]. With regard to NSAIDs-loaded nanoparticles, there are few studies about in vivo toxicology and no clinical assays have been performed yet. Flurbiprofen-loaded nanoparticles of both polymers, PLGA [59] and Eudragit [74], were applied to rabbit eyes according to the Draize test [226], showing no sign of toxicity or irritation to ocular tissues. Diclofenac-loaded nanoparticles produced with PLGA, PACA or PCL were studied by a modified Draize test, with the in vivo results showing no sign of irritation or damaging effects to ocular tissues in rabbit eyes for as long as 24 h after application [227]. In an in vivo study using rabbit eye, Eudragit nanosuspension containing 0.1% ibuprofen showed a very good ocular tolerability [73, 228]. Moreover, in vitro cell viability studies and in vivo Draize test show non-irritant properties of Dexibuprofen PLGA-PEG nanospheres [229].
D
Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Dexibuprofen is the S(+)-enantiomer of ibuprofen. After metabolic transformation in the liver (hydroxylation and carboxylation), the pharmacologically inactive metabolites are completely excreted, mainly by the kidneys (90%), but also in the bile.
Clinical pharmacology: traditional NSAIDs and selective COX-2 inhibitors
Published in Pamela E Macintyre, Suellen M Walker, David J Rowbotham, Clinical Pain Management, 2008
Stephen F Jones, Aidan M O’Donnell
Ibuprofen was developed in 1964 as a safer alternative to aspirin in the treatment of rheumatoid arthritis. It was the first NSAID after aspirin licenced for over-the-counter use in the UK (1983) and the USA (1984). In common with other drugs in this class, ibuprofen contains a chiral carbon in the alpha position of the propionate moiety, which gives rise to two enantiomers of the molecule. It has been found that (S)-(+)-ibuprofen (dexibuprofen) is the active enantiomer both in vitro and in vivo. However, further testing has revealed an isomerase which converts inactive (R)-ibuprofen to the active (S)-enantiomer in vivo. Despite this, dexibuprofen preparations are available in many countries. Enantiomeric conversion varies widely between individuals, which may partly explain why plasma concentrations do not equate to analgesic efficacy.90
Formulation of solid dispersion to improve dissolution and oral bioavailability of poorly soluble dexibuprofen
Published in Pharmaceutical Development and Technology, 2021
Dexibuprofen (DEXI) (S-2-(4-isobutyl phenyl)-propionic acid), a nonsteroidal anti-inflammatory drug, is typically used in the treatment of osteoarthritis, acute and chronic pain, rheumatoid arthritis, and related conditions (Bondan et al. 2017; Gordo et al. 2017; Ho et al. 2018). DEXI is an S+ enantiomer of ibuprofen and belongs to Biopharmaceutics Classification System class II with low solubility (around 11 µg/mL) and high permeability (Kaehler et al. 2003; Rinaki et al. 2004; Potthast et al. 2005; Tsume et al. 2012; Stoyanova et al. 2016). The high permeability of ibuprofen and its enantiomers have been observed in Caco-2 cell cultures. In a radiolabeled Caco-2 cell culture study, the apparent permeability coefficient (Papp) of ibuprofen was 30.1 × 10−6 cm/s (Berben et al. 2018). Due to its low solubility, the dissolution rate of DEXI is limited in the GI tract, thereby decreasing the BA of the drug. Thus, improving the solubility and dissolution rate of DEXI can enhance the BA of the drug. Therefore, several techniques have been developed to improve the drug solubility and BA (Karashima et al. 2017; Ahsan and Verma 2018; Choi et al. 2019a).
Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect
Published in Drug Development and Industrial Pharmacy, 2019
Yoonho Choi, Kyoung Ah Min, Chong-Kook Kim
Based on these considerations, in the present study, the immediate-release formulation of dexibuprofen was optimized with various ratios of hydrophilic carrier excipients to drug compound for studies including aqueous solubility and dissolution testing in the physiological medium. Then, by encapsulating the immediate-release form (solid dispersion) and sustained-release formulation in hard gelatin capsules, we designed a new oral dosage form of dexibuprofen for the controlled-release. Finally, the in vivo absorption potential of the novel dexibuprofen formulations, as compared to that of dexibuprofen powder, was examined by a comparative pharmacokinetic study in rats,. This study is the first attempt to formulate the combined oral dosage form of dexibuprofen by using a solid dispersion preparation and a sustained-release formula to relieve pain with a fast onset and an extended manner of action.
Postoperative pain: a review of emerging therapeutic options
Published in Expert Review of Neurotherapeutics, 2021
Abhishek K Gupta, Shayla Mena, Zhaosheng Jin, Tong J Gan, Sergio Bergese
For instance, researchers that synthesized dexibuprofen nanocrystals, found the analgesic effects of the nanocrystals to occur at lower doses (5 mg/kg) that than of two controls, standard dexibuprofen (40 mg/kg) and diclofenac sodium (20 mg/kg) [174]. Dexibuprofen itself, is an S (+)-isomer of ibuprofen that has equivalent analgesic effects to ibuprofen, but with a lower probability of producing adverse gastric effects. Similarly, dexketoprofen is associated with less injection site reaction than ketoprofen [175]. Nanocrystal formulation of other drugs such as meloxicam are also under study [176].