Synthesis and structure–property evaluation of cellulose ω-carboxyesters for amorphous solid dispersions

Liu, Haoyu; Ilevbare, Grace A.; Cherniawski, Benjamin P.; Ritchie, Earl T.; Taylor, Lynne S.; Edgar, Kevin J.

doi:10.1016/j.carbpol.2012.11.049

Cited by 54 publications

(73 citation statements)

References 30 publications

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“…Poly(2‐vinyl pyridine), linear with a MW of approximately 40,000 Da was purchased from Scientific Polymer Products Inc. (Ontario, New York). Carboxymethyl cellulose acetate butyrate (CMCAB) ( M w 35,000 Da) was obtained from Eastman Chemical Company (Kingsport, Tennessee) and cellulose propionate adipate (CAPAdp) was synthesized by our collaborators at Virginia Tech University. Model compounds and model polymers are depicted in Figures and .…”

Section: Methodsmentioning

confidence: 99%

Trends in the Precipitation and Crystallization Behavior of Supersaturated Aqueous Solutions of Poorly Water-Soluble Drugs Assessed Using Synchrotron Radiation

Raina

Eerdenbrugh

Alonzo

et al. 2015

Journal of Pharmaceutical Sciences

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Section: Methodsmentioning

confidence: 99%

Trends in the Precipitation and Crystallization Behavior of Supersaturated Aqueous Solutions of Poorly Water-Soluble Drugs Assessed Using Synchrotron Radiation

Raina

Eerdenbrugh

Alonzo

et al. 2015

Journal of Pharmaceutical Sciences

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“…2 Currently, $60% of NCEs discovered are poorly water soluble or lipophilic in nature. 3,4 According to the Biopharmaceutical Classification System (BCS) of drugs, these compounds typically belong to the BCS class II (low solubility-high permeability). 5 Absorption of such compounds are solubility-or dissolution rate-limited.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of the aqueous solubility and permeability of a poorly water soluble drug ritonavir via lyophilized milk-based solid dispersions

Dhore

Dave

Saoji

et al. 2016

Pharmaceutical Development and Technology

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In the present study, a lyophilized milk-based solid dispersion (SD) of ritonavir (RTV) was developed with the goal of improving its aqueous solubility. The SD was prepared by lyophilization, and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy and powder X-ray diffraction (PXRD) were used to confirm the formation and robustness of the SD formulation. The prepared SD formulations were functionally evaluated by saturation solubility, in vitro drug release and ex vivo permeation studies. The optimized SD formulation exhibited a significantly higher (30-fold) aqueous solubility (11.36 ± 0.06 μg/mL), compared to the pure RTV (0.37 ± 0.03 μg/mL). The in vitro dissolution studies revealed a significantly higher (∼10-fold) efficiency of the optimized SD formulation in releasing the RTV, compared to the pure RTV. The ex vivo permeation studies with the everted intestine method showed that prepared SD formulation significantly improved the permeation of RTV (75.6 ± 3.09, % w/w), compared to pure RTV (20.45 ± 1.68, % w/w). Thus, SD formulation utilizing lyophilized milk as a carrier appears to be a promising alternative strategy to improve the aqueous solubility of poorly water soluble drugs.

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“…Researchers have designed new cellulose derivatives in the hopes of achieving a balance in the properties needed for an effective single polymer ASD system . However, criteria like hydrophilicity for enhanced drug release versus hydrophobicity for enhanced polymer–drug interactions may conflict with one another, challenging the polymer designer.…”

Section: Introductionmentioning

confidence: 99%

“…Recent studies in our laboratories have highlighted the effectiveness of polymer blends composed of novel cellulosic polymers including suberate, adipate, and sebacate esters of cellulose acetate propionate mixed with commercial cellulose‐based and synthetic polymers. Blending two moderately hydrophobic cellulosic polymers, or combining a hydrophobic cellulosic polymer with a more hydrophilic synthetic polymer, afforded synergistic crystal growth inhibition of the poorly soluble CYP‐3A4 inhibitor ritonavir …”

Section: Introductionmentioning

confidence: 99%

“…28 Researchers have designed new cellulose derivatives in the hopes of achieving a balance in the properties needed for an effective single polymer ASD system. 23 However, criteria like hydrophilicity for enhanced drug release versus hydrophobicity for enhanced polymer-drug interactions may conflict with one another, challenging the polymer designer. Therefore, polymer blending may be an attractive alternative for dealing with deficiencies of existing or novel drug delivery polymers, including those for ASD.…”

Section: Introductionmentioning

confidence: 99%

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Pairwise Polymer Blends for Oral Drug Delivery

Marks

Wegiel

Taylor

et al. 2014

Journal of Pharmaceutical Sciences

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Blends of polymers with complementary properties hold promise for addressing the diverse, demanding polymer performance requirements in amorphous solid dispersions (ASDs), but we lack comprehensive property understanding for blends of important ASD polymers. Herein, we prepare pairwise blends of commercially available polymers polyvinylpyrrolidone (PVP), the cationic acrylate copolymer Eudragit 100 (E100), hydroxypropyl methylcellulose acetate succinate (HPMCAS), carboxymethyl cellulose acetate butyrate (CMCAB), hydroxypropyl methylcellulose (HPMC), and the new derivative cellulose acetate adipate propionate (CAAdP). This study identifies miscible binary blends that may find use, for example, in ASDs for solubility and bioavailability enhancement of poorly water-soluble drugs. Differential scanning calorimetry, FTIR spectroscopy, and film clarity were used to determine blend miscibility. Several polymer combinations including HPMCAS/PVP, HPMC/CMCAB, and PVP/HPMC appear to be miscible in all proportions. In contrast, blends of E100/PVP and E100/HPMC showed a miscibility gap. Combinations of water-soluble and hydrophobic polymers like these may permit effective balancing of ASD performance criteria such as release rate and polymer-drug interaction to prevent nucleation and crystal growth of poorly soluble drugs. Miscible polymer combinations described herein will enable further study of their drug delivery capabilities, and provide a potentially valuable set of ASD formulation tools.

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Synthesis and structure–property evaluation of cellulose ω-carboxyesters for amorphous solid dispersions

Cited by 54 publications

References 30 publications

Trends in the Precipitation and Crystallization Behavior of Supersaturated Aqueous Solutions of Poorly Water-Soluble Drugs Assessed Using Synchrotron Radiation

Trends in the Precipitation and Crystallization Behavior of Supersaturated Aqueous Solutions of Poorly Water-Soluble Drugs Assessed Using Synchrotron Radiation

Enhancement of the aqueous solubility and permeability of a poorly water soluble drug ritonavir via lyophilized milk-based solid dispersions

Pairwise Polymer Blends for Oral Drug Delivery

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