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Kurihara, Atsushi; Shibayama, Yoko; Mizota, Atsuko; Yasuno, Akiko; Ikeda, Miyoshi; Sasagawa, Kazuhiko; Kobayashi, T.; Hisaoka, Masafumi

doi:10.1023/a:1016063719541

Cited by 23 publications

(2 citation statements)

References 8 publications

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“…The potential pharmaceutical applications include use as a carrier for lipophilic drugs [7][8][9][10][11] and for site-specific drug delivery by attaching ligands for various cell surface receptors to the particle surface. 12) Generally, intravenous emulsions are biodegradable, biocompatible, physically stable, easy to scale up and cost effective when compared to other drug carriers.…”

mentioning

confidence: 99%

Formulation, Characterization and Hypersensitivity Evaluation of an Intravenous Emulsion Loaded with a Paclitaxel-Cholesterol Complex

Xia

Guo

Liu

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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The objective of this paper was to develop a novel Cremophor-free, autoclave stable, intravenous emulsion for paclitaxel (PACE). A paclitaxel-cholesterol complex was used as the drug carrier to improve the solubility of paclitaxel in the oil phase of emulsions. The complex and PACE were prepared by rotary evaporation and highpressure homogenization, respectively. Effects of oil phases, emulsifiers and pH values on the characteristics of PACE were investigated. PACE was characterized with regard to its appearance, morphology, osmolality, pH value, particle size, zeta potential, encapsulation efficiency and stability. Hypersensitivity was evaluated by guinea pig hypersensitivity reaction. The final formulation was composed of the complex, soybean oil, mediumchain triglyceridel, soybean lecithin, poloxamer 188 and glycerol. The resulting PACE had an encapsulation efficiency of 97.3% with a particle size of 135 nm and a zeta potential of ؊38.3 mV. Osmolality and pH of the formulation were 383 mOsmol/kg and 4.5, respectively. The formulation survived autoclaving at 115°C for 30 min and remained stable for at least 12 months at 6°C. PACE also exhibited a better tolerance than an equal dose of Cremophor-based paclitaxel injection in guinea pigs, as no obvious hypersensitivity reaction was observed. These results suggested that PACE has a great potential for industrial-scale production and clinical applications.

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confidence: 99%

Formulation, Characterization and Hypersensitivity Evaluation of an Intravenous Emulsion Loaded with a Paclitaxel-Cholesterol Complex

Xia

Guo

Liu

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Studies have revealed larger sized droplets (>250 nm compared to <100 nm) were cleared faster from the body, indicating a great role of mononuclear phagocyte system (MPS) in the clearance of these nanoemulsion [29]. Moreover, droplet size has also been demonstrated to determine the intratumor distribution versus the peripheral tissues [30]. Therefore, it is in common agreement that nanoemulsions with mean droplet size of less than 150 nm and a narrow, unimodal distribution is highly favored.…”

Section: Nanoemulsionmentioning

confidence: 94%

Utilizing 505(b)(2) Regulatory Pathway for New Drug Applications: An Overview on the Advanced Formulation Approach and Challenges

Chen¹,

Zhang²,

Wang³

et al. 2023

Drug Repurposing - Advances, Scopes and Opportunities in Drug Discovery

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More than 50% of approved drugs on the market contain poorly water-soluble APIs, which typically are associated with poor bioavailability, suboptimal drug delivery, ineffective drug efficacy, and side effects. This creates a huge opportunity in generating 505(b)(2) products, which address unmet medical needs by applying formulation technologies to overcome those difficulties. A key feature of the 505(b)(2) pathway is the 505(b)(2) sponsor can rely upon clinical data or literature produced by other companies. The 505(b)(2) pathway allows manufacturers to acquire FDA approval without performing all the work required with a traditional NDA. The 505(b)(2) strategy can be an option to improve existing drug products with a new indication, dosage form, dosing regimen, strength, combination with other products, new route of administration, elimination of food effect, switching from a prescription drugs (Rx) to an over-the-counter (OTC), non-prescription product that differs from the OTC monograph, and orphan drug indications. Both generic and brand companies are turning to more complex 505(b)(2) products to avoid the commoditized generic competition. Revitalization of older marketed drug products using innovative drug delivery technologies or platforms can provide new marketing exclusivity and new patent protection, and thus offer an effective tool for product life cycle management.

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Enhanced absorption and drug targeting by positively charged submicron emulsions

Yang

Benita

2000

Drug Dev. Res.

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Abstract: When particle size is properly selected, these emulsions could be promising and effective as an injectable carrier for lipophilic antitumor agents in order to enhance the tumor delivery and efficacies while reducing toxicities.

Cited by 23 publications

References 8 publications

Formulation, Characterization and Hypersensitivity Evaluation of an Intravenous Emulsion Loaded with a Paclitaxel-Cholesterol Complex

Formulation, Characterization and Hypersensitivity Evaluation of an Intravenous Emulsion Loaded with a Paclitaxel-Cholesterol Complex

Utilizing 505(b)(2) Regulatory Pathway for New Drug Applications: An Overview on the Advanced Formulation Approach and Challenges

Enhanced absorption and drug targeting by positively charged submicron emulsions

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