Gaurav K Jain, Gaurav Chaudhary, Mohammad Akhlaquer Rahman, Musarrat Husain Warsi, Mohammad Imran
{"title":"纳米化和推进剂辅助雾化表面修饰提高雌二醇的溶解度和溶解性。","authors":"Gaurav K Jain, Gaurav Chaudhary, Mohammad Akhlaquer Rahman, Musarrat Husain Warsi, Mohammad Imran","doi":"10.1208/s12249-025-03151-2","DOIUrl":null,"url":null,"abstract":"<p><strong>Objective: </strong>A novel method for the development of uniform, nanosized, crystalline particles of estradiol valerate (EV) by the propellant assisted aerosolization (PAA) technique as an alternative to supercritical carbon dioxide assisted atomization is described.</p><p><strong>Methods: </strong>HFA 134a was used as a propellant. PAA process parameters such as nozzle diameter, pre-expansion pressure, and hot air pressure were optimized using 33 factorial Box-Behnken design for the preparation of uniform, nanosized EV (nano-EV). Nano-EV was characterized for physicochemical properties, crystallinity and enhancement of the solubility and dissolution.</p><p><strong>Results: </strong>The nano-EV, produced by the PAA technique, showed loose cuboidal aggregates with smooth surface morphology. PAA with 0.22 µm nozzle diameter, 120 psi pre-expansion pressure and 80 psi hot air pressure, yielded uniform (PDI, 0.27 ± 0.05) nano-EV particles with mean size of about 291 ± 5.8 nm. FTIR and DSC confirmed that no physical or chemical change occurred during nanosizing. XRD data showed that nano-EV particles were crystalline. The results demonstrated nearly twofold higher solubility and 2.3-fold enhanced dissolution of nano-EV compared to EV.</p><p><strong>Conclusion: </strong>The PAA process is a cost effective and scalable technique and has a potential industrial application for producing nanocrystals of BCS class II drugs.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 5","pages":"165"},"PeriodicalIF":3.4000,"publicationDate":"2025-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Nanosizing and Surface Modification by Propellant Assisted Aerosolization Enhances Solubility and Dissolution of Estradiol.\",\"authors\":\"Gaurav K Jain, Gaurav Chaudhary, Mohammad Akhlaquer Rahman, Musarrat Husain Warsi, Mohammad Imran\",\"doi\":\"10.1208/s12249-025-03151-2\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objective: </strong>A novel method for the development of uniform, nanosized, crystalline particles of estradiol valerate (EV) by the propellant assisted aerosolization (PAA) technique as an alternative to supercritical carbon dioxide assisted atomization is described.</p><p><strong>Methods: </strong>HFA 134a was used as a propellant. PAA process parameters such as nozzle diameter, pre-expansion pressure, and hot air pressure were optimized using 33 factorial Box-Behnken design for the preparation of uniform, nanosized EV (nano-EV). Nano-EV was characterized for physicochemical properties, crystallinity and enhancement of the solubility and dissolution.</p><p><strong>Results: </strong>The nano-EV, produced by the PAA technique, showed loose cuboidal aggregates with smooth surface morphology. PAA with 0.22 µm nozzle diameter, 120 psi pre-expansion pressure and 80 psi hot air pressure, yielded uniform (PDI, 0.27 ± 0.05) nano-EV particles with mean size of about 291 ± 5.8 nm. FTIR and DSC confirmed that no physical or chemical change occurred during nanosizing. XRD data showed that nano-EV particles were crystalline. The results demonstrated nearly twofold higher solubility and 2.3-fold enhanced dissolution of nano-EV compared to EV.</p><p><strong>Conclusion: </strong>The PAA process is a cost effective and scalable technique and has a potential industrial application for producing nanocrystals of BCS class II drugs.</p>\",\"PeriodicalId\":6925,\"journal\":{\"name\":\"AAPS PharmSciTech\",\"volume\":\"26 5\",\"pages\":\"165\"},\"PeriodicalIF\":3.4000,\"publicationDate\":\"2025-06-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"AAPS PharmSciTech\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1208/s12249-025-03151-2\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"AAPS PharmSciTech","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1208/s12249-025-03151-2","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Nanosizing and Surface Modification by Propellant Assisted Aerosolization Enhances Solubility and Dissolution of Estradiol.
Objective: A novel method for the development of uniform, nanosized, crystalline particles of estradiol valerate (EV) by the propellant assisted aerosolization (PAA) technique as an alternative to supercritical carbon dioxide assisted atomization is described.
Methods: HFA 134a was used as a propellant. PAA process parameters such as nozzle diameter, pre-expansion pressure, and hot air pressure were optimized using 33 factorial Box-Behnken design for the preparation of uniform, nanosized EV (nano-EV). Nano-EV was characterized for physicochemical properties, crystallinity and enhancement of the solubility and dissolution.
Results: The nano-EV, produced by the PAA technique, showed loose cuboidal aggregates with smooth surface morphology. PAA with 0.22 µm nozzle diameter, 120 psi pre-expansion pressure and 80 psi hot air pressure, yielded uniform (PDI, 0.27 ± 0.05) nano-EV particles with mean size of about 291 ± 5.8 nm. FTIR and DSC confirmed that no physical or chemical change occurred during nanosizing. XRD data showed that nano-EV particles were crystalline. The results demonstrated nearly twofold higher solubility and 2.3-fold enhanced dissolution of nano-EV compared to EV.
Conclusion: The PAA process is a cost effective and scalable technique and has a potential industrial application for producing nanocrystals of BCS class II drugs.
期刊介绍：
AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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