Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of Valsartan
Solubility is an essential criterion for attaining desired concentration of the drug within the systemic circulation to ensure intended pharmacological action. The main setback for the formulation development of new chemical entities and generic drugs is their lower aqueous solubility. Therefore, a...
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| Format: | Article |
| Language: | English |
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Elsevier
2023-12-01
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| Series: | Applied Surface Science Advances |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2666523923001587 |
| _version_ | 1797389430090104832 |
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| author | Muhammad Suhail Muhammad Usman Minhas Abid Naeem Syed Faisal Badshah Kifayat Ullah Khan Muhammad Fahad Pao-Chu Wu |
| author_facet | Muhammad Suhail Muhammad Usman Minhas Abid Naeem Syed Faisal Badshah Kifayat Ullah Khan Muhammad Fahad Pao-Chu Wu |
| author_sort | Muhammad Suhail |
| collection | DOAJ |
| description | Solubility is an essential criterion for attaining desired concentration of the drug within the systemic circulation to ensure intended pharmacological action. The main setback for the formulation development of new chemical entities and generic drugs is their lower aqueous solubility. Therefore, a drug carrier system is needed which not only enhances the solubility of low aqueous soluble drugs but also maintains a constant pharmacological action of drugs within predetermined intervals of time. For this purpose, authors prepared carbopol 934-co-poly(itaconic acid) (CPcPIA) nanogels by the free radical polymerization technique for the solubility enhancement of Valsartan. The polymeric nanogels were characterized and studied for further evaluation. FTIR studies indicated no interactions between the drug and nanogel contents. SEM showed a porous and sponged structure of particles without any agglomeration. Similarly, higher thermal stability was detected for the fabricated nanogel compared to its constituents, while reduction in crystallinity of the drug and excipients was shown by XRD analysis, indicating the amorphous nature of the polymeric nanogels. Average particle size and zeta potential of prepared nanogels were found 290.32 nm and –8.32 mV, respectively. Furthermore, various studies such as sol-gel fraction, dynamic swelling, drug loading, in-vitro drug release studies, solubility, and toxicity study were conducted for the developed nanogels. A significant increase in the solubility of Valsartan (2.002, 2.976, and 3.543 mg/mL) was observed by polymeric nanogels in pH 1.2, deionized distilled water, and pH 7.4 as compared to reference product. Toxicity study indicated no toxic effect of prepared nanogels on rabbit's species. Thus, it can be demonstrated from the results that synthesized nanogels are not only limited to a specific class of drug but the solubility of all low aqueous soluble drugs can be enhanced by the prepared networks of nanogels. |
| first_indexed | 2024-03-08T22:55:50Z |
| format | Article |
| id | doaj.art-aa4c2922fa904341bc9d3afd9f304b4e |
| institution | Directory Open Access Journal |
| issn | 2666-5239 |
| language | English |
| last_indexed | 2024-03-08T22:55:50Z |
| publishDate | 2023-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Applied Surface Science Advances |
| spelling | doaj.art-aa4c2922fa904341bc9d3afd9f304b4e2023-12-16T06:09:36ZengElsevierApplied Surface Science Advances2666-52392023-12-0118100524Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of ValsartanMuhammad Suhail0Muhammad Usman Minhas1Abid Naeem2Syed Faisal Badshah3Kifayat Ullah Khan4Muhammad Fahad5Pao-Chu Wu6Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Punjab 63100, PakistanFaculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Punjab 63100, Pakistan; College of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan; Corresponding author at: Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Punjab 63100, Pakistan.Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Punjab 63100, PakistanDepartment of Pharmacy, Faculty of Medical and Health Sciences, University of Poonch, Azad Jammu and Kashmir, Rawalakot 10250, PakistanQuaid-e-Azam College of Pharmacy, Sahiwal, PakistanFaculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Punjab 63100, PakistanSchool of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 807, Taiwan, ROC; Department of Medical Research, Kaohsiung Medical University Hospital, Kaohsiung City 80708, Taiwan, ROC; Drug Development and Value Creation Research Center, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan, ROC; Corresponding author at: School of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 80708, Taiwan, ROC.Solubility is an essential criterion for attaining desired concentration of the drug within the systemic circulation to ensure intended pharmacological action. The main setback for the formulation development of new chemical entities and generic drugs is their lower aqueous solubility. Therefore, a drug carrier system is needed which not only enhances the solubility of low aqueous soluble drugs but also maintains a constant pharmacological action of drugs within predetermined intervals of time. For this purpose, authors prepared carbopol 934-co-poly(itaconic acid) (CPcPIA) nanogels by the free radical polymerization technique for the solubility enhancement of Valsartan. The polymeric nanogels were characterized and studied for further evaluation. FTIR studies indicated no interactions between the drug and nanogel contents. SEM showed a porous and sponged structure of particles without any agglomeration. Similarly, higher thermal stability was detected for the fabricated nanogel compared to its constituents, while reduction in crystallinity of the drug and excipients was shown by XRD analysis, indicating the amorphous nature of the polymeric nanogels. Average particle size and zeta potential of prepared nanogels were found 290.32 nm and –8.32 mV, respectively. Furthermore, various studies such as sol-gel fraction, dynamic swelling, drug loading, in-vitro drug release studies, solubility, and toxicity study were conducted for the developed nanogels. A significant increase in the solubility of Valsartan (2.002, 2.976, and 3.543 mg/mL) was observed by polymeric nanogels in pH 1.2, deionized distilled water, and pH 7.4 as compared to reference product. Toxicity study indicated no toxic effect of prepared nanogels on rabbit's species. Thus, it can be demonstrated from the results that synthesized nanogels are not only limited to a specific class of drug but the solubility of all low aqueous soluble drugs can be enhanced by the prepared networks of nanogels.http://www.sciencedirect.com/science/article/pii/S2666523923001587Solubility enhancementNanogelsCorbopolValsartanToxicity evaluation |
| spellingShingle | Muhammad Suhail Muhammad Usman Minhas Abid Naeem Syed Faisal Badshah Kifayat Ullah Khan Muhammad Fahad Pao-Chu Wu Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of Valsartan Applied Surface Science Advances Solubility enhancement Nanogels Corbopol Valsartan Toxicity evaluation |
| title | Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of Valsartan |
| title_full | Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of Valsartan |
| title_fullStr | Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of Valsartan |
| title_full_unstemmed | Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of Valsartan |
| title_short | Preparation, characterization, in-vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of Valsartan |
| title_sort | preparation characterization in vitro and toxicological evaluation of carbopol based nanogels for solubility enhancement of valsartan |
| topic | Solubility enhancement Nanogels Corbopol Valsartan Toxicity evaluation |
| url | http://www.sciencedirect.com/science/article/pii/S2666523923001587 |
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