Article
Chemistry, Medicinal
Sonal Bhujbal, Vaibhav Pathak, Dmitry Y. Zemlyanov, Lynne S. Taylor, Qi (Tony) Zhou
Summary: This study developed amorphous solid dispersion (ASD) of lumefantrine using a cost-effective spray anti-solvent precipitation method, studying four acidic polymers as excipients at different drug-polymer ratios. The results showed that HPMCP and HPMCAS-based ASDs exhibited the best physical stability and drug release levels.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Sathish Dharani, Eman M. Mohamed, Tahir Khuroo, Ziyaur Rahman, Mansoor A. Khan
Summary: This study aimed to improve the physicochemical properties and oral bioavailability of dasatinib by using the amorphous solid dispersion approach. The results showed that the ASD formulation significantly increased dissolution and oral bioavailability compared to the physical mixture.
Article
Medicine, Research & Experimental
Dana E. Moseson, Lynne S. Taylor
Summary: This Perspective article discusses the origin and significance of crystallinity within amorphous solid dispersions and the complex impact it can have on drug performance. The importance of comprehensive assessment of sample properties is emphasized, and various factors to consider in ASD formulations are discussed.
MOLECULAR PHARMACEUTICS
(2023)
Article
Chemistry, Medicinal
Yiru Wang, Yudan Fang, Feng Zhou, Qi Liang, Yueyi Deng
Summary: Among the three polymers used as carriers for amorphous solid dispersions of quercetin, HPMCAS-HF showed the highest ability to inhibit quercetin crystallization and maintain supersaturation. The release behavior of the prepared solid dispersions depended on polymer-quercetin interactions and the polymer's ability to inhibit crystallization.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Chemistry, Medicinal
Nitprapa Siriwannakij, Tycho Heimbach, Abu T. M. Serajuddin
Summary: This study investigates the incomplete drug release from amorphous solid dispersions (ASDs), finding that ritonavir does not completely dissolve in aqueous media, forming supersaturated solutions. The excess drug is dispersed in an oily amorphous form with low particle sizes. Accelerated stability testing confirms the physical stability of the extrudates.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Edina Szabo, Anna Haraszti, Petra Zahonyi, Daniel Vadas, Istvan Csontos, Zsombor Kristof Nagy, Guy Van den Mooter, Gyorgy Marosi
Summary: The aim of this research was to investigate three thermoanalytical techniques for determining the glass transition temperature (T-g). The results showed that T-g values measured by thermally stimulated depolarization currents had higher deviation from theoretical calculations than those measured by modulated differential scanning calorimetry. Micro-thermal analysis proved to be the most sensitive in detecting changes in T-g values and indicating sample instability. The study also emphasized the importance of active pharmaceutical ingredient content in the stability of ASDs.
Article
Chemistry, Medicinal
Sichen Song, Chenguang Wang, Bo Zhang, Changquan Calvin Sun, Timothy P. Lodge, Ronald A. Siegel
Summary: This study reports a method of miscibility determination based on the overlap concentration, c*, which can be conveniently determined from the viscosity-composition diagram. The determined c* values strongly correlate with the physical stability of amorphous solid dispersions (ASDs) of two model drugs, celecoxib and loratadine, with four different grades of polyvinylpyrrolidone (PVP). This suggests the potential application of the c* concept in designing stable high drug loaded ASD formulations and provides a procedure for broader adoption of this methodology, which is easy to apply and widely applicable for thermally stable binary drug/polymer combinations.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Review
Pharmacology & Pharmacy
Sai Krishna Anand Vullendula, Athira R. Nair, Dani Lakshman Yarlagadda, K. S. Navya Sree, Krishnamurthy Bhat, Swapnil J. Dengale
Summary: This review critically compares polymeric amorphous solid dispersion and co-amorphous technology based on improvement in drug loading, stability, solubility, dissolution, and bioavailability. It finds that polymeric dispersions outperform co-amorphous materials in terms of physical stability and bioavailability, while co-amorphous materials tend to possess high drug loadings. Both polymeric solid dispersion and co-amorphous systems show similar performance in terms of supersaturation and processability.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Polymer Science
Arif Budiman, Neng Vera Nurani, Eli Laelasari, Muchtaridi Muchtaridi, Sriwidodo Sriwidodo, Diah Lia Aulifa
Summary: This study aimed to characterize the interaction between a drug and polymer in amorphous solid dispersions (ASDs) and evaluate the impact on the physical stability and dissolution of alpha-mangostin (AM). The presence of polymers significantly improved the solubility and dissolution rate of AM, but the extent of this improvement varied depending on the polymer and storage conditions.
Review
Polymer Science
Arif Budiman, Annisa Luthfiyah Handini, Mutia Nur Muslimah, Neng Vera Nurani, Eli Laelasari, Insan Sunan Kurniawansyah, Diah Lia Aulifa
Summary: Improving the solubility of anticancer drugs for oral administration is crucial for enhancing their efficacy and safety. Amorphous solid dispersion (ASD) is a promising approach to increase the aqueous solubility and bioavailability of poorly water-soluble drugs. This study summarizes and elucidates the mechanisms and impact of the ASD system on cancer therapy, providing a comprehensive overview and discussion of related issues.
Article
Medicine, Research & Experimental
Mohammad Atif Faiz Afzal, Kristin Lehmkemper, Ekaterina Sobich, Thomas F. Hughes, David J. Giesen, Teng Zhang, Caroline M. Krauter, Paul Winget, Matthias Degenhardt, Samuel O. Kyeremateng, Andrea R. Browning, John C. Shelley
Summary: Amorphous solid dispersions (ASDs) are commonly used for oral delivery of poorly water-soluble small-molecule drugs. Producing a high-performance ASD involves considering factors such as drug solubility in the matrix and drug release rate in aqueous medium. Molecular dynamics simulations provide unique insights into the dissolution behavior mechanisms of ASDs. The study shows that polymer microstructures and drug-polymer interactions play important roles in the dissolution behavior of ASDs.
MOLECULAR PHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Masafumi Fukiage, Kyosuke Suzuki, Maki Matsuda, Yohei Nishida, Michinori Oikawa, Takuya Fujita, Kohsaku Kawakami
Summary: This study explored the preparation of naftopidil ASDs using different materials, revealing the potential occurrence of LLPS during dissolution, and finding that Eudragit ASD, despite poor dissolution behavior, offered the best oral absorption.
Article
Pharmacology & Pharmacy
Chenhui Wang, Xiaowei Liu, Ruihan Zhao, Meiqing Yang, Wenqian Liu, Qiuyang Dai, Xiaofeng Bao, Yong Chen, Jun Ma
Summary: This study aimed to improve the dissolution and oral bioavailability of chrysin by developing a stable solid dispersion formulation. The optimized solid dispersion showed enhanced dissolution rates and had acceptable stability. In rat models, the solid dispersion of chrysin exhibited stronger antihyperlipidemic effects compared to chrysin raw material.
Article
Medicine, Research & Experimental
Isha Saraf, Robert Roskar, Dattatray Modhave, Michael Brunsteiner, Anjali Karn, Dmytro Neshchadin, Georg Gescheidt, Amrit Paudel
Summary: The study investigated the oxidative degradation behavior of NIF in ASDs prepared with different chain lengths of PVP. Short chain PVP K30 led to more severe drug degradation compared to long chain PVP K90. The drug-polymer intermolecular interactions were found to influence the oxidative degradation process, as supported by electronic structure calculations and experimental results.
MOLECULAR PHARMACEUTICS
(2022)
Review
Pharmacology & Pharmacy
Jinghan Li, Yihan Wang, Dongyue Yu
Summary: Polymeric amorphous solid dispersion (ASD) is a commonly used method to improve the solubility of poorly water-soluble drugs. The addition of a secondary excipient, such as a second polymer, counterions, or surfactants, can further enhance the stability and dissolution performance of ASDs. Different polymers in a combination ASD serve unique functions, while in situ salt formation increases the glass transition temperature and surfactants improve wettability. However, the potential negative effects of surfactants on stability and dissolution need to be carefully considered. Additionally, externally added excipients, such as magnesium stearate and inorganic salts, can have an impact on the solid-state stability and dissolution of ASD tablets.