Formulation and in vitro Evaluation of Acemetacin Nanosuspension
Acemetacin (ACM) is classified as a non-steroidal anti-inflammatory drug (NSAID). It is an indomethacin glycolic ester that is transformed into indomethacin in vivo. The analgesic, antipyretic, and anti-inflammatory properties of the ACM are attributed to its prostaglandin inhibitory action. Acemet...
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College of Pharmacy University of Baghdad
2025-02-01
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| Series: | Iraqi Journal of Pharmaceutical Sciences |
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| Online Access: | https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/3561 |
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| author | Hussein Al-Gharani Khalid Al-Kinani |
| author_facet | Hussein Al-Gharani Khalid Al-Kinani |
| author_sort | Hussein Al-Gharani |
| collection | DOAJ |
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Acemetacin (ACM) is classified as a non-steroidal anti-inflammatory drug (NSAID). It is an indomethacin glycolic ester that is transformed into indomethacin in vivo. The analgesic, antipyretic, and anti-inflammatory properties of the ACM are attributed to its prostaglandin inhibitory action. Acemetacin belongs to biopharmaceutical classification system (BCS) class II drugs, which are characterized by having high permeability but poor aqueous solubility. The purpose of this study was to develop acemetacin nanoparticles (ACM NPs) for enhanced solubility and rate of dissolution. The solvent-anti-solvent approach was used to formulate the nanoparticles. Two stabilizers were used to prepare ACM NPs (sodium deoxycholate (SDC) and Soluplus®). Design Expert® software was used to create the experiments utilizing a computer-based approach. The Box-Behnken design was used for this purpose in order to investigate the effect of different formulation variables on particle size and polydispersity index (PDI) of ACM NPs. Using Soluplus® as a stabilizer, the chosen formula F22 has desirability value 0.701, and its particle size and PDI values were 59.69 nm and 0.1847 respectively. The saturated solubility of ACM in the generated nanoparticles was approximately ten times greater than that of the naked drug (25.01 μg/ml vs. 2.43 μg/ml), and a 100% dissolution was accomplished in 90 minutes compared to the naked ACM, which only gave 47% in this time frame. In conclusion, this is the first time reporting the preparation of ACM nanosuspension, and turning ACM into polymeric nanoparticles is an effective method to increase the solubility and rate of dissolution of the drug, readying it for incorporation into a dosage form requiring such properties.
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| format | Article |
| id | doaj-art-98719cb87c194475a808309bc28c8e90 |
| institution | DOAJ |
| issn | 1683-3597 2521-3512 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | College of Pharmacy University of Baghdad |
| record_format | Article |
| series | Iraqi Journal of Pharmaceutical Sciences |
| spelling | doaj-art-98719cb87c194475a808309bc28c8e902025-08-20T02:48:28ZengCollege of Pharmacy University of BaghdadIraqi Journal of Pharmaceutical Sciences1683-35972521-35122025-02-0133(4SI)10.31351/vol33iss(4SI)pp133-146Formulation and in vitro Evaluation of Acemetacin NanosuspensionHussein Al-Gharani0Khalid Al-Kinani1Ministry of Health and Environment, Karbala Health Directorate, Karbala, IraqDepartment of Pharmaceutics, College of Pharmacy ,University of Baghdad, Baghdad, Iraq Acemetacin (ACM) is classified as a non-steroidal anti-inflammatory drug (NSAID). It is an indomethacin glycolic ester that is transformed into indomethacin in vivo. The analgesic, antipyretic, and anti-inflammatory properties of the ACM are attributed to its prostaglandin inhibitory action. Acemetacin belongs to biopharmaceutical classification system (BCS) class II drugs, which are characterized by having high permeability but poor aqueous solubility. The purpose of this study was to develop acemetacin nanoparticles (ACM NPs) for enhanced solubility and rate of dissolution. The solvent-anti-solvent approach was used to formulate the nanoparticles. Two stabilizers were used to prepare ACM NPs (sodium deoxycholate (SDC) and Soluplus®). Design Expert® software was used to create the experiments utilizing a computer-based approach. The Box-Behnken design was used for this purpose in order to investigate the effect of different formulation variables on particle size and polydispersity index (PDI) of ACM NPs. Using Soluplus® as a stabilizer, the chosen formula F22 has desirability value 0.701, and its particle size and PDI values were 59.69 nm and 0.1847 respectively. The saturated solubility of ACM in the generated nanoparticles was approximately ten times greater than that of the naked drug (25.01 μg/ml vs. 2.43 μg/ml), and a 100% dissolution was accomplished in 90 minutes compared to the naked ACM, which only gave 47% in this time frame. In conclusion, this is the first time reporting the preparation of ACM nanosuspension, and turning ACM into polymeric nanoparticles is an effective method to increase the solubility and rate of dissolution of the drug, readying it for incorporation into a dosage form requiring such properties. https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/3561Acemetacin nanoparticles, Solvent-anti-solvent, Box-Behnken design. |
| spellingShingle | Hussein Al-Gharani Khalid Al-Kinani Formulation and in vitro Evaluation of Acemetacin Nanosuspension Iraqi Journal of Pharmaceutical Sciences Acemetacin nanoparticles, Solvent-anti-solvent, Box-Behnken design. |
| title | Formulation and in vitro Evaluation of Acemetacin Nanosuspension |
| title_full | Formulation and in vitro Evaluation of Acemetacin Nanosuspension |
| title_fullStr | Formulation and in vitro Evaluation of Acemetacin Nanosuspension |
| title_full_unstemmed | Formulation and in vitro Evaluation of Acemetacin Nanosuspension |
| title_short | Formulation and in vitro Evaluation of Acemetacin Nanosuspension |
| title_sort | formulation and in vitro evaluation of acemetacin nanosuspension |
| topic | Acemetacin nanoparticles, Solvent-anti-solvent, Box-Behnken design. |
| url | https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/3561 |
| work_keys_str_mv | AT husseinalgharani formulationandinvitroevaluationofacemetacinnanosuspension AT khalidalkinani formulationandinvitroevaluationofacemetacinnanosuspension |