Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres
Lu Shan,1 En-Xue Tao,2 Qing-Hui Meng,3 Wen-Xia Hou,3 Kang Liu,1 Hong-Cai Shang,4 Jin-Bao Tang,1 Wei-Fen Zhang1,4 1School of Pharmacy, Weifang Medical University, 2The Affiliated Hospital of Weifang Medical University, 3School of Nursing, Weifang Medical University, Weifang, 4Key Laboratory of Chine...
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| Format: | Article |
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Dove Medical Press
2016-01-01
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| Series: | Drug Design, Development and Therapy |
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| Online Access: | https://www.dovepress.com/formulation-optimization-and-pharmacodynamic-evaluation-of-chitosanpho-peer-reviewed-article-DDDT |
| _version_ | 1818652767961481216 |
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| author | Shan L Tao EX Meng QH Hou WX Liu K Shang HC Tang JB Zhang WF |
| author_facet | Shan L Tao EX Meng QH Hou WX Liu K Shang HC Tang JB Zhang WF |
| author_sort | Shan L |
| collection | DOAJ |
| description | Lu Shan,1 En-Xue Tao,2 Qing-Hui Meng,3 Wen-Xia Hou,3 Kang Liu,1 Hong-Cai Shang,4 Jin-Bao Tang,1 Wei-Fen Zhang1,4 1School of Pharmacy, Weifang Medical University, 2The Affiliated Hospital of Weifang Medical University, 3School of Nursing, Weifang Medical University, Weifang, 4Key Laboratory of Chinese Internal Medicine of Ministry of Education and Beijing, Dongzhimen Hospital, Beijing University of Chinese Medicine, Beijing, People’s Republic of China Abstract: Cholinergic neurotransmission loss is the main cause of cognitive impairment in patients with Alzheimer’s disease. Phospholipids (PLs) play an essential role in memory and learning abilities. Moreover, PLs act as a source of choline in acetylcholine synthesis. This study aimed to prepare and optimize the formulation of chitosan/phospholipid/β-cyclodextrin (CTS/PL/β-CD) microspheres that can improve cognitive impairment. The CTS/PL/β-CD microspheres were prepared by spray drying, and optimized with an orthogonal design. These microspheres were also characterized in terms of morphology, structure, thermostability, drug loading, and encapsulation efficiency. The spatial learning and memory of rats were evaluated using the Morris water maze test, and the neuroprotective effects of the CTS/PL/β-CD microspheres were investigated by immunohistochemistry. Scanning electron microscopic images showed that the CTS/PL/β-CD microspheres were spherical with slightly wrinkled surfaces. Fourier transform infrared spectroscopy and differential scanning calorimetry proved that PLs formed hydrogen bonds with the amide group of CTS and the hydroxyl group of β-CD. The learning and memory abilities of rats in the treated group significantly improved compared with those in the model group. Immunohistochemical analysis revealed that treatment with the CTS/PL/β-CD microspheres attenuated the expression of protein kinase C-δ and inhibited the activation of microglias. These results suggest that the optimized microspheres have the potential to be used in the treatment of Alzheimer’s disease. Keywords: chitosan, spray drying, microsphere, Alzheimer’s disease, phospholipids |
| first_indexed | 2024-12-17T02:27:15Z |
| format | Article |
| id | doaj.art-2fee21a4e43a439ebd67191dde49c9c6 |
| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-12-17T02:27:15Z |
| publishDate | 2016-01-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Drug Design, Development and Therapy |
| spelling | doaj.art-2fee21a4e43a439ebd67191dde49c9c62022-12-21T22:07:04ZengDove Medical PressDrug Design, Development and Therapy1177-88812016-01-012016Issue 141742925352Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheresShan LTao EXMeng QHHou WXLiu KShang HCTang JBZhang WFLu Shan,1 En-Xue Tao,2 Qing-Hui Meng,3 Wen-Xia Hou,3 Kang Liu,1 Hong-Cai Shang,4 Jin-Bao Tang,1 Wei-Fen Zhang1,4 1School of Pharmacy, Weifang Medical University, 2The Affiliated Hospital of Weifang Medical University, 3School of Nursing, Weifang Medical University, Weifang, 4Key Laboratory of Chinese Internal Medicine of Ministry of Education and Beijing, Dongzhimen Hospital, Beijing University of Chinese Medicine, Beijing, People’s Republic of China Abstract: Cholinergic neurotransmission loss is the main cause of cognitive impairment in patients with Alzheimer’s disease. Phospholipids (PLs) play an essential role in memory and learning abilities. Moreover, PLs act as a source of choline in acetylcholine synthesis. This study aimed to prepare and optimize the formulation of chitosan/phospholipid/β-cyclodextrin (CTS/PL/β-CD) microspheres that can improve cognitive impairment. The CTS/PL/β-CD microspheres were prepared by spray drying, and optimized with an orthogonal design. These microspheres were also characterized in terms of morphology, structure, thermostability, drug loading, and encapsulation efficiency. The spatial learning and memory of rats were evaluated using the Morris water maze test, and the neuroprotective effects of the CTS/PL/β-CD microspheres were investigated by immunohistochemistry. Scanning electron microscopic images showed that the CTS/PL/β-CD microspheres were spherical with slightly wrinkled surfaces. Fourier transform infrared spectroscopy and differential scanning calorimetry proved that PLs formed hydrogen bonds with the amide group of CTS and the hydroxyl group of β-CD. The learning and memory abilities of rats in the treated group significantly improved compared with those in the model group. Immunohistochemical analysis revealed that treatment with the CTS/PL/β-CD microspheres attenuated the expression of protein kinase C-δ and inhibited the activation of microglias. These results suggest that the optimized microspheres have the potential to be used in the treatment of Alzheimer’s disease. Keywords: chitosan, spray drying, microsphere, Alzheimer’s disease, phospholipidshttps://www.dovepress.com/formulation-optimization-and-pharmacodynamic-evaluation-of-chitosanpho-peer-reviewed-article-DDDTChitosanSpray dryingMicrosphereADPhospholipids |
| spellingShingle | Shan L Tao EX Meng QH Hou WX Liu K Shang HC Tang JB Zhang WF Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres Drug Design, Development and Therapy Chitosan Spray drying Microsphere AD Phospholipids |
| title | Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres |
| title_full | Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres |
| title_fullStr | Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres |
| title_full_unstemmed | Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres |
| title_short | Formulation, optimization, and pharmacodynamic evaluation of chitosan/phospholipid/β-cyclodextrin microspheres |
| title_sort | formulation optimization and pharmacodynamic evaluation of chitosan phospholipid beta cyclodextrin microspheres |
| topic | Chitosan Spray drying Microsphere AD Phospholipids |
| url | https://www.dovepress.com/formulation-optimization-and-pharmacodynamic-evaluation-of-chitosanpho-peer-reviewed-article-DDDT |
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