Improved Corneal Toxicity and Permeability of Tranilast by the Preparation of Ophthalmic Formulations Containing Its Nanoparticles

Nagai, Noriaki; Ono, Hikaru; Hashino, Miho; Ito, Yoshimasa; Okamoto, Norio; Shimomura, Yoshikazu

doi:10.5650/jos.ess13082

Cited by 38 publications

(55 citation statements)

References 31 publications

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“…It will be interesting to observe what benefits these innovative drug preparations can provide to patients. In addition, we describe a new method for preparing drug solid nanoparticles established by us [30][31][32].The particle size of our drug solid nanoparticles is of high quality (particle size, approximately 60-80 nm). Dispersions containing these drug nanoparticles are tolerated better by human and rat corneal epithelial cells than commercially available eye drops, since the accumulation of drug in nanoparticles is lower than from solutions.…”

Section: Resultsmentioning

confidence: 99%

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A New Preparation Method for Ophthalmic Drug Nanoparticles

Nagai

Ito²

2014

Pharm Anal Acta

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Section: Resultsmentioning

confidence: 99%

“…We have also designed ophthalmic formulations containing drug nanoparticles obtained by mill methods [30,31]. Ophthalmic solutions containing indomethacin (IMC) solid nanoparticles (IMC nano ) were prepared using zirconia beads and Bead Smash 12 (a bead mill, Wakenyaku Co. Ltd, Kyoto, Japan) (Figure 1).…”

Section: Preparation Of Ocular Drug Nanomaterialsmentioning

confidence: 99%

A New Preparation Method for Ophthalmic Drug Nanoparticles

Nagai

Ito²

2014

Pharm Anal Acta

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“…23,24) Zirconia beads (diameter: 2 mm) were added to the IMC microparticles with or without MC, and the mixtures were crushed with the Bead Smash 12 for 30 s (3000 rpm, 4°C). The mixtures were then dispersed in saline with or without 5% HPβCD, and crushed again with the Bead Smash 12 (5500 rpm, 30 s×15 times, 4°C) in the presence of zirconia beads (diameter: 0.1 mm).…”

Section: Animals and Materialsmentioning

confidence: 99%

“…Mori et al 36) reported that adsorption to the surface of cyclodextrin decreases the cohesion of nanoparticulate solids, and we previously reported that the addition of HPβCD to the mixture is suitable for the preparation of nanoparticles using mill methods. 23,24) Therefore, we attempted to prepare an IMC dispersion containing 0.5% MC and 5% HPβCD using the bead mill method. HPβCD was found to enhance the stability of the IMC dispersion (IMC nano ), and no precipitation was observed 14 d after preparation (Table 1).…”

Section: Gastric and Small Intestinal Ulcerogenic Response To Imc In mentioning

confidence: 99%

“…[19][20][21][22] On the other hand, we have also developed methods to prepare tranilast solid nanoparticles by a bead mill method, and showed that these solid nanoparticles enhance drug bioavailability. 23,24) It is possible that decreasing the amount of orally administered NSAIDs by improving their bioavailability may lead to an expansion of their usage as therapy for RA patients.…”

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confidence: 99%

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Effect of Solid Nanoparticle of Indomethacin on Therapy for Rheumatoid Arthritis in Adjuvant-Induced Arthritis Rat

Nagai

Ito

2014

Biological & Pharmaceutical Bulletin

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We designed new oral formulations containing indomethacin (IMC) solid nanoparticles, and investigate their usefulness by evaluating bioavailability and gastrointestinal lesions. The IMC solid nanoparticles were prepared using methylcellulose (MC), 2-hydroxypropyl-β-cyclodextrin (HPβCD), and the bead mill method, and high quality dispersions containing 1.0% IMC nanoparticles were prepared (IMC nano , particle size: 76 58 nm, means S.D.). The fate of serum IMC and the induction of paw edema in adjuvant-induced arthritis (AA) rats receiving low-doses IMC nano (0.4 mg/kg) were similar to those following the administration of a therapeutic dose of conventional IMC prepared with MC and HPβCD (conventional IMC, 2 mg/kg), and the bioavailability in 0.4 mg/kg IMC nano was 5.3-fold higher in comparison with that in 2 mg/kg conventional IMC. IMC-induced gastrointestinal lesions in AA rats administered IMC nano (8 mg/kg), in consideration of bioavailability, were significantly less than for conventional IMC (40 mg/kg). On the other hand, the toxicity caused by conventional IMC and IMC nano was similar in Caco-2 cells. It is possible that the oral administration of IMC solid nanoparticles will show increased effectiveness in treating RA without causing IMC-induced gastrointestinal lesions, since the bioavailability is higher than that of conventional IMC. An oral drug delivery system using drug nanoparticles may expand the usage of NSAIDs for therapy in the inflammatory field.

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Nanocrystal for ocular drug delivery: hope or hype

Sharma

Patel

Mehta

2016

Drug Deliv. and Transl. Res.

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The complexity of the structure and nature of the eye emanates a challenge for drug delivery to formulation scientists. Lower bioavailability concern of conventional ocular formulation provokes the interest of researchers in the development of novel drug delivery system. Nanotechnology-based formulations have been extensively investigated and found propitious in improving bioavailability of drugs by overcoming ocular barriers prevailing in the eye. The advent of nanocrystals helped in combating the problem of poorly soluble drugs specifically for oral and parenteral drug delivery and led to development of various marketed products. Nanocrystal-based formulations explored for ocular drug delivery have been found successful in achieving increase in retention time, bioavailability, and permeability of drugs across the corneal and conjunctival epithelium. In this review, we have highlighted the ocular physiology and barriers in drug delivery. A comparative analysis of various nanotechnology-based ocular formulations is done with their pros and cons. Consideration is also given to various methods of preparation of nanocrystals with their patented technology. This article highlights the success achieved in conquering various challenges of ocular delivery by the use of nanocrystals while emphasizing on its advantages and application for ocular formulation. The perspectives of nanocrystals as an emerging flipside to explore the frontiers of ocular drug delivery are discussed.

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Improved Corneal Toxicity and Permeability of Tranilast by the Preparation of Ophthalmic Formulations Containing Its Nanoparticles

Cited by 38 publications

References 31 publications

A New Preparation Method for Ophthalmic Drug Nanoparticles

A New Preparation Method for Ophthalmic Drug Nanoparticles

Effect of Solid Nanoparticle of Indomethacin on Therapy for Rheumatoid Arthritis in Adjuvant-Induced Arthritis Rat

Nanocrystal for ocular drug delivery: hope or hype

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