Development and characterization of an organic solvent free, proliposomal formulation of Busulfan using quality by design approach

Chobisa, Dhawal; Patel, Ketan; Monpara, Jasmin; Patel, Mayank R.; Vavia, Pradeep R.

doi:10.1016/j.ijpharm.2017.11.007

Cited by 13 publications

(2 citation statements)

References 31 publications

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“…The results of the saturation solubility of Retro-2 in different cosolvent systems (DMA, PG, and PEG-400) suggested that DMA is the most suitable cosolvent for the preparation of Retro-2 loaded SNEDDS. Also, we designed a formulation incorporating DMA into SNEDDS, because previously, DMA has been investigated as a promising cosolvent in preparation of SNEDDS because of its low viscosity, high drug solubilization capacity, biocompatibility, and emulsifying property. , The solubility of Retro-2 in Captex 300 was found to be 1.2 mg/mL. A high solubility of Retro-2 in DMA helped in enhancing drug loading in the preconcentrate.…”

Section: Discussionmentioning

confidence: 99%

Development of an Arginine Anchored Nanoglobule with Retrograde Trafficking Inhibitor (Retro-2) for the Treatment of an Enterohemorrhagic Escherichia coli Outbreak

et al. 2019

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Enterohemorrhagic Escherichia coli O157:H7 (EHEC) or Shiga toxin-producing E. coli (STEC) is known to cause sporadic and epidemic gastrointestinal infections with several incidences of outbreaks. Antibiotic-based therapy further worsens the condition by facilitating the release of Shiga toxins (Stx) and lipopolysaccharides (LPS). Hence, there is an urgent need to develop an antibiotic-free, safe, and effective therapeutic intervention for the treatment of EHEC infections. We proposed a novel therapeutic strategy to address this clinical problemkill, capture, and inhibit. We aimed to formulate and characterize lauroyl arginate ethyl ester (LAE) and Retro-2 loaded self-nano emulsifying drug delivery systems (SNEDDS). Retro-2 is a recently developed novel class of molecule, which can selectively inhibit retrograde transport of Stx. In this paper, we first carried out preformulation studies of Retro-2, followed by the development of SNEDDS forming arginine anchored nanoglobules (AR-NG), characterization of LPS binding to AR-NG, and finally evaluation of activity against EHEC. Retro-2 showed extremely poor solubility at all gastrointestinal pH values, susceptibility to acidic environments, and good permeability. The positively charged AR-NG spontaneously formed a globule size of 102.8 ± 1.9 nm with a surface charge of +52.15 ± 3 mV and increased the solubility of Retro-2. Further, binding and aggregation of LPS and AR-NG were confirmed by particle size, polydispersity index, zeta potential, fluorescent intensity, turbidity analysis, and a limulus amebocyte lysate (LAL) test. Additionally, a significant reduction in LPS induced TNF-α was observed in AR-NG treated macrophages. Thus, in this paper, we demonstrate a very promising and innovative therapeutic approach based on the “kill (E. Coli), capture (released LPS), and inhibit (transport of Stx)” concept.

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Section: Discussionmentioning

confidence: 99%

Development of an Arginine Anchored Nanoglobule with Retrograde Trafficking Inhibitor (Retro-2) for the Treatment of an Enterohemorrhagic Escherichia coli Outbreak

et al. 2019

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“…Therefore, to find out an effective method to stabilize and solubilize busulfan is practical demand. Some work on improving the solubility of busulfan are reported, [2] but enhancing stability is still difficult [1,3] …”

Section: Introductionmentioning

confidence: 99%

Stabilization of Antitumor Agent Busulfan through Encapsulation within a Water‐Soluble Pillar[5]arene

Hui-feng

Huang

Dong

et al. 2022

Chemistry An Asian Journal

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The complexation of the antitumor agent busulfan by negatively charged carboxylatopillar[5]arene in water is reported. The encapsulation within carboxylatopillar[5]arene reduces the hydrolytic degradation of busulfan from 90.7% to 25.2% after 24 days and accordingly enhances its stability by providing a hydrophobic shelter for busulfan in water. Moreover, the complexation results in 12 times improvement of water solubility for busulfan. Our result provides a supramolecular approach for stabilizing the anticancer agent busulfan.

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Application of quality by design in optimization of nanoformulations: Principle, perspectives and practices

Birla,

Khandale,

Bashir

et al. 2024

Drug Deliv. and Transl. Res.

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Development and characterization of an organic solvent free, proliposomal formulation of Busulfan using quality by design approach

Cited by 13 publications

References 31 publications

Development of an Arginine Anchored Nanoglobule with Retrograde Trafficking Inhibitor (Retro-2) for the Treatment of an Enterohemorrhagic Escherichia coli Outbreak

Development of an Arginine Anchored Nanoglobule with Retrograde Trafficking Inhibitor (Retro-2) for the Treatment of an Enterohemorrhagic Escherichia coli Outbreak

Stabilization of Antitumor Agent Busulfan through Encapsulation within a Water‐Soluble Pillar[5]arene

Application of quality by design in optimization of nanoformulations: Principle, perspectives and practices

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