The effect of drug loading on the properties of abiraterone–hydroxypropyl beta cyclodextrin solid dispersions processed by solvent free KinetiSol® technology

Gala, Urvi; Miller, Dave A.; Su, Yongchao; Spangenberg, Angela; Williams, Robert O.

doi:10.1016/j.ejpb.2021.05.001

Cited by 14 publications

(7 citation statements)

References 57 publications

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“…A further example of the usefulness of the HETCOR technique in the identification of the spatial correlations between API and polymer was given in the stability of the structure of the abiraterone-hydroxypropyl-β-cyclodextrin dispersion 77 prepared by an innovative solvent-free technology known as KinetiSol. 78 The 1 H– 13 C HETCOR showed a clear interaction between the aromatic region of the abiraterone and the anomeric protons of the cyclodextrin.…”

Section: D Correlation Nmr Experiments As a Toolkit To Probe Api–poly...mentioning

confidence: 99%

New Development in Understanding Drug–Polymer Interactions in Pharmaceutical Amorphous Solid Dispersions from Solid-State Nuclear Magnetic Resonance

et al. 2022

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Pharmaceutical amorphous solid dispersions (ASDs) represent a widely used technology to increase the bioavailability of active pharmaceutical ingredients (APIs). ASDs are based on an amorphous API dispersed in a polymer, and their stability is driven by the presence of strong intermolecular interactions between these two species (e.g., hydrogen bond, electrostatic interactions, etc.). The understanding of these interactions at the atomic level is therefore crucial, and solid-state nuclear magnetic resonance (NMR) has demonstrated itself as a very powerful technique for probing API−polymer interactions. Other reviews have also reported exciting approaches to study the structures and dynamic properties of ASDs and largely focused on the study of API−polymer miscibility and on the identification of API−polymer interactions. Considering the increased use of NMR in the field, the aim of this Review is to specifically highlight recent experimental strategies used to identify API−polymer interactions and report promising recent examples using one-dimensional (1D) and two-dimensional (2D) experiments by exploiting the following emerging approaches of very-high magnetic field and ultrafast magic angle spinning (MAS). A range of different ASDs spanning APIs and polymers with varied structural motifs is targeted to illustrate new ways to understand the mechanism of stability of ASDs to enable the design of new dispersions.

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Section: D Correlation Nmr Experiments As a Toolkit To Probe Api–poly...mentioning

confidence: 99%

New Development in Understanding Drug–Polymer Interactions in Pharmaceutical Amorphous Solid Dispersions from Solid-State Nuclear Magnetic Resonance

et al. 2022

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“…According to the Noyes-Whitney equation and Ostwald-Freundlich equation, the nanocrystal could significantly enhance the surface area compared to raw materials leading to a huge improvement in dissolution rate [26,27]. At the same time, nanocrystals prepared with fewer types of excipients exhibit in vivo safety with good stability and are suitable for various administration routes such as oral delivery, injection delivery, ocular delivery, pulmonary delivery, and intramuscular injection [28][29][30][31][32][33]. The new technology is considered as the potential solution to effectively improve drug dissolution and absorption.…”

Section: Scheme 1 (A)mentioning

confidence: 99%

Development of Abiraterone Acetate Nanocrystal Tablets to Enhance Oral Bioavailability: Formulation Optimization, Characterization, In Vitro Dissolution and Pharmacokinetic Evaluation

Liu

et al. 2022

Pharmaceutics

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Abiraterone acetate is a prodrug of abiraterone used in combination with prednisone as a standard therapeutic strategy for hormone-resistant prostate cancer (mCRPC). Due to the poor solubility and permeability, the release and absorption of abiraterone acetate are low and reduce its bioavailability. In this project, abiraterone acetate tablets prepared using nanocrystal technology were developed to overcome the drawbacks of normal tablets by enhancing in vitro dissolution rate and oral bioavailability. The abiraterone acetate nanocrystal suspensions were prepared by top-down wet milling method using a planetary ball mill with the mixture of Poloxamer 407 and Poloxamer 188 as the optimized stabilizer at a ratio of 7:1. The optimized nanocrystals were freeze-dried and characterized using DLS, TEM, DSC, and XRD. The abiraterone acetate nanocrystal tablets significantly improve the in vitro dissolution rate of abiraterone acetate compared to raw materials. Although exhibiting a similar dissolution rate compared to the Zytiga® tablets, the nanocrystal tablets significantly improve the oral bioavailability with Cmax and AUC0–t being 3.51-fold and 2.80-fold higher, respectively, in the pharmacokinetic study. The present data indicate that nanocrystal is a promising strategy for improving the dissolution and bioavailability of abiraterone acetate.

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“…Any unexpected discrepancies within the process will affect the quality of entire batch materials within the batch manufacturing process. The batch manufacturing process involves testing various in-process or intermediate products to ensure the quality of the product [73][74][75]. The finished product manufactured by batch manufacturing requires complete testing and release of the product from the quarantine before being distributed into the market.…”

Section: Coupling Of Hme and Fdm 3d Printing Processmentioning

confidence: 99%

A review of hot melt extrusion paired fused deposition modeling three-dimensional printing for developing patient centric dosage forms

Dhoppalapudi¹,

Illa²

2022

GSC Biol. Pharm. Sci.

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In recent years, the demand for developing patient-centric dosage forms is increasing enormously with the increasing patient population. Much research is ongoing exploring various additive manufacturing techniques for developing pharmaceutical medications. Poor solubility of drug substances and underdeveloped manufacturing strategies are majorly affecting the pharmaceutical industry's revenue. Developing intravenous dosage forms for drug substances with poor solubility will affect the revenue of the pharmaceutical industries. Thus, improving solubility remains to be the major prerequisite for the developmental scientist. In addition to improving solubility, establishing a robust manufacturing process with commercial viability is also essential. In recent years hot melt extrusion (HME) has been most widely investigated for developing amorphous solid dispersions (ASDs) over other techniques such as spray drying and KinetisolÒ. The process of HME can be coupled with the fused deposition modeling (FDM) three-dimensional (3D) printing technique which is capable of fabricating on-demand patient-centric dosage forms. A continuous manufacturing line can be established by painting HME and FDM 3D printing processes. The quality of the product can be controlled and monitored by employing suitable process analytical technology (PAT) tools. Though the process of the HME-paired FDM 3D printing process has resulted in various advantages compared to the conventional manufacturing process, still many limitations, such as the limited number of polymers, reproducibility, and stability, need to be addressed.

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The effect of drug loading on the properties of abiraterone–hydroxypropyl beta cyclodextrin solid dispersions processed by solvent free KinetiSol® technology

Cited by 14 publications

References 57 publications

New Development in Understanding Drug–Polymer Interactions in Pharmaceutical Amorphous Solid Dispersions from Solid-State Nuclear Magnetic Resonance

New Development in Understanding Drug–Polymer Interactions in Pharmaceutical Amorphous Solid Dispersions from Solid-State Nuclear Magnetic Resonance

Development of Abiraterone Acetate Nanocrystal Tablets to Enhance Oral Bioavailability: Formulation Optimization, Characterization, In Vitro Dissolution and Pharmacokinetic Evaluation

A review of hot melt extrusion paired fused deposition modeling three-dimensional printing for developing patient centric dosage forms

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