Brimonidine Tartrate–Eudragit Long-Acting Nanoparticles: Formulation, Optimization, In Vitro and In Vivo Evaluation

Bhagav, Prakash; Upadhyay, Hariom; Chandran, Sajeev

doi:10.1208/s12249-011-9675-1

Cited by 81 publications

(38 citation statements)

References 34 publications

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“…For both groups, normal saline was administered in the same location of the right eye. Results showed that the nanoparticles were well tolerated, with no signs of irritation or toxicity 17. Moreover, the BRT nanoparticles decreased the elevated IOP in rabbits with glaucoma for a longer period of time compared to the conventional drop formulation (p<0.0001) 17…”

Section: Resultsmentioning

confidence: 94%

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Nanotechnology and glaucoma: a review of the potential implications of glaucoma nanomedicine

et al. 2013

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The purpose of this review is to discuss the evolution of nanotechnology and its potential diagnostic and therapeutic applications in the field of ophthalmology, particularly as it pertains to glaucoma. We reviewed literature using MEDLINE and PubMed databases with the following search terms: glaucoma, nanotechnology, nanomedicine, nanoparticles, ophthalmology and liposomes. We also reviewed pertinent references from articles found in this search. A brief history of nanotechnology and nanomedicine will be covered, followed by a discussion of the advantages and concerns of using this technology in the field of glaucoma. We will look at various studies concerning the development of nanomedicine, its potential applications in ocular drug delivery, diagnostic and imaging modalities and, surgical techniques. In particular, the challenges of assuring safety and efficacy of nanomedicine will be examined. We conclude that nanotechnology offers a novel approach to expanding diagnostic, imaging and surgical modalities in glaucoma and may contribute to the knowledge of disease pathogenesis at a molecular level. However, more research is needed to better elucidate the mechanism of cellular entry, the potential for nanoparticle cytotoxicity and the assurance of clinical efficacy.

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Section: Resultsmentioning

confidence: 94%

“…Bhagav and colleagues used brimonidine tartrate (BRT) encapsulated Eudragit nanoparticles to study prolonged release of BRT 17. The Eudragit nanoparticles are inert polymeric resin copolymers used to entrap lipophilic drugs.…”

Section: Resultsmentioning

confidence: 99%

Nanotechnology and glaucoma: a review of the potential implications of glaucoma nanomedicine

et al. 2013

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“…Dialysis sacs are also used in combination with official USP dissolution/release apparatus (such as USP apparatus 1 and 2). For example, a dialysis sac method was used in the USP apparatus 1 (basket type) to study brimonidine tartrate release from Eudragit long acting nanoparticles (26). This study demonstrated that brimonidine tartrate release from the nanoparticles was controlled by non-Fickian anomalous transport, which was very valuable to assist in formulation optimization to achieve the desired drug release behavior (26).…”

Section: Current In Vitro Dissolution/release Testing Methodsmentioning

confidence: 99%

“…For example, a dialysis sac method was used in the USP apparatus 1 (basket type) to study brimonidine tartrate release from Eudragit long acting nanoparticles (26). This study demonstrated that brimonidine tartrate release from the nanoparticles was controlled by non-Fickian anomalous transport, which was very valuable to assist in formulation optimization to achieve the desired drug release behavior (26). However, due to the hindrance to drug diffusion through the dialysis membranes as well as the lack of adequate agitation inside the dialysis sacs themselves, violation of sink conditions has been reported (13, 19, 27, 28).…”

Section: Current In Vitro Dissolution/release Testing Methodsmentioning

confidence: 99%

In vitro dissolution testing strategies for nanoparticulate drug delivery systems: recent developments and challenges

Shen

Burgess

2013

Drug Deliv. and Transl. Res.

151

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Nanoparticulate systems have emerged as prevalent drug delivery systems over the past few decades. These delivery systems (such as liposomes, emulsions, nanocrystals, and polymeric nanocarriers) have been extensively used to improve bioavailability, prolong pharmacological effects, achieve targeted drug delivery, as well as reduce side effects. Considering that any unanticipated change in product performance of such systems may result in toxicity and/or change in vivo efficacy, it is essential to develop suitable in vitro dissolution/release testing methods to ensure product quality and performance, and to assist in product development. The present review provides an overview of the current in vitro dissolution/release testing methods such as dialysis, sample and separate, as well as continuous flow methods. Challenges and future directions in the development of standardized and biorelevant in vitro dissolution/release testing methods for novel nanoparticulate systems are discussed.

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“…The latter is cationic copolymer synthesized from acrylic acid and methacrylic acid esters with 5% quaternary ammonium groups (16). Like Eudragit® RL100, Eudragit® RS100 is able to develop stable non-irritant nano-dispersions suitable for ocular drug delivery (17)(18)(19).…”

Section: Introductionmentioning

confidence: 99%

Positively Charged Polymeric Nanoparticle Reservoirs of Terbinafine Hydrochloride: Preclinical Implications for Controlled Drug Delivery in the Aqueous Humor of Rabbits

et al. 2013

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Abstract. Frequent instillation of terbinafine hydrochloride (T HCl) eye drops (0.25%, w/v) is necessary to maintain effective aqueous humor concentrations for treatment of fungal keratitis. The current approach aimed at developing potential positively charged controlled-release polymeric nanoparticles (NPs) of T HCl. The estimation of the drug pharmacokinetics in the aqueous humor following ocular instillation of the best-achieved NPs in rabbits was another goal. Eighteen drug-loaded (0.50%, w/v) formulae were fabricated by the nanopreciptation method using Eudragit® RS100 and chitosan (0.25%, 0.5%, and 1%, w/v). Soybean lecithin (1%, w/v) and Pluronic® F68 (0.5%, 1%, and 1.5%, w/v) were incorporated in the alcoholic and aqueous phases, respectively. The NPs were evaluated for particle size, zeta potential, entrapment efficiency percentage (EE%), morphological examination, drug release in simulated tear fluid (pH 7.4), Fourier-transform IR (FT-IR), X-ray diffraction (XRD), physical stability (2 months, 4°C and 25°C), and drug pharmacokinetics in the rabbit aqueous humor relative to an oily drug solution. Spherical, discrete NPs were successfully developed with mean particle size and zeta potential ranging from 73.29 to 320.15 nm and +20.51 to +40.32 mV, respectively. Higher EE% were achieved with Eudragit® RS100-based NPs. The duration of drug release was extended to more than 8 h. FT-IR and XRD revealed compatibility between inactive formulation ingredients and T HCl and permanence of the latter's crystallinity, respectively. The NPs were physically stable, for at least 2 months, when refrigerated. F5-NP suspension significantly (P<0.05) increased drug mean residence time and improved its ocular bioavailability; 1.657-fold.

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Brimonidine Tartrate–Eudragit Long-Acting Nanoparticles: Formulation, Optimization, In Vitro and In Vivo Evaluation

Cited by 81 publications

References 34 publications

Nanotechnology and glaucoma: a review of the potential implications of glaucoma nanomedicine

Nanotechnology and glaucoma: a review of the potential implications of glaucoma nanomedicine

In vitro dissolution testing strategies for nanoparticulate drug delivery systems: recent developments and challenges

Positively Charged Polymeric Nanoparticle Reservoirs of Terbinafine Hydrochloride: Preclinical Implications for Controlled Drug Delivery in the Aqueous Humor of Rabbits

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