Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids
Objective(s): Curcuminoids, comprising curcumin, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), are bioactive phytochemicals with numerous pharmacological effects. Oral biological availability of curcuminoids is low due to the low aqueous solubility and rapid metabolism. This study aimed a...
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| Format: | Article |
| Language: | English |
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Mashhad University of Medical Sciences
2019-03-01
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| Series: | Iranian Journal of Basic Medical Sciences |
| Subjects: | |
| Online Access: | http://ijbms.mums.ac.ir/article_12252_d7c8c914cdd8434f0a317a16dc3bcb10.pdf |
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| author | Mahdi Hatamipour Amirhossein Sahebkar Seyedeh Hoda Alavizadeh Mahyar Dorri Mahmoud Reza Jaafari |
| author_facet | Mahdi Hatamipour Amirhossein Sahebkar Seyedeh Hoda Alavizadeh Mahyar Dorri Mahmoud Reza Jaafari |
| author_sort | Mahdi Hatamipour |
| collection | DOAJ |
| description | Objective(s): Curcuminoids, comprising curcumin, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), are bioactive phytochemicals with numerous pharmacological effects. Oral biological availability of curcuminoids is low due to the low aqueous solubility and rapid metabolism. This study aimed at fabricating a nanomicellar curcuminoid formula with enhanced pharmacokinetic properties. Materials and Methods: Curcuminoids nanomicelles were prepared and characterized regarding particle properties, stability, release profile and pharmacokinetic parameters.Results: Encapsulation efficiency of curcuminoids in nanomicelles were 100%. Particle size analysis demonstrated a mean size of around 10 nm that remained stable for 24 months. Dissolution test showed the complete dissolution of encapsulated curcuminoids from nanomicelles within 20 min while the free curcuminoids were poorly dissolved (approximately 7% after 60 min). The results of long-term (24 months) and accelerated (6 months) stability studies showed no changes in the size and content of nanomicelles. The release studies in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) showed no release of curcuminoids for at least 4 hours. In vivo study in BALB/c mice showed improved pharmacokinetic parameters including maximum plasma concentration (Cmax) and time to reach the maximum concentration (Tmax) with nanomicelles as compared to free curcuminoids and two other commercial products. Tmax for all the three curcuminoid components was observed 30 min following oral administration. AUC of nanomicellar curcuminoids was 59.2 times more than free curcuminoids. Conclusion: These data indicated that nanomicelles could improve solubility, oral bioavailability and also the stability of curcuminoids. Thus, they merit further investigation for enhancing pharmacological effects of curcuminoids. |
| first_indexed | 2024-12-12T05:10:07Z |
| format | Article |
| id | doaj.art-bdc1ff3456b94e37b42fc9f977dc005a |
| institution | Directory Open Access Journal |
| issn | 2008-3866 2008-3874 |
| language | English |
| last_indexed | 2024-12-12T05:10:07Z |
| publishDate | 2019-03-01 |
| publisher | Mashhad University of Medical Sciences |
| record_format | Article |
| series | Iranian Journal of Basic Medical Sciences |
| spelling | doaj.art-bdc1ff3456b94e37b42fc9f977dc005a2022-12-22T00:36:58ZengMashhad University of Medical SciencesIranian Journal of Basic Medical Sciences2008-38662008-38742019-03-0122328228910.22038/ijbms.2019.32873.785212252Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoidsMahdi Hatamipour0Amirhossein Sahebkar1Seyedeh Hoda Alavizadeh2Mahyar Dorri3Mahmoud Reza Jaafari4Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran|Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, IranBiotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran|Neurogenic Inflammation Research Center, Mashhad University of Medical Sciences, Mashhad, IranNanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran|Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, IranNanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran|Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, IranNanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran|Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, IranObjective(s): Curcuminoids, comprising curcumin, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), are bioactive phytochemicals with numerous pharmacological effects. Oral biological availability of curcuminoids is low due to the low aqueous solubility and rapid metabolism. This study aimed at fabricating a nanomicellar curcuminoid formula with enhanced pharmacokinetic properties. Materials and Methods: Curcuminoids nanomicelles were prepared and characterized regarding particle properties, stability, release profile and pharmacokinetic parameters.Results: Encapsulation efficiency of curcuminoids in nanomicelles were 100%. Particle size analysis demonstrated a mean size of around 10 nm that remained stable for 24 months. Dissolution test showed the complete dissolution of encapsulated curcuminoids from nanomicelles within 20 min while the free curcuminoids were poorly dissolved (approximately 7% after 60 min). The results of long-term (24 months) and accelerated (6 months) stability studies showed no changes in the size and content of nanomicelles. The release studies in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) showed no release of curcuminoids for at least 4 hours. In vivo study in BALB/c mice showed improved pharmacokinetic parameters including maximum plasma concentration (Cmax) and time to reach the maximum concentration (Tmax) with nanomicelles as compared to free curcuminoids and two other commercial products. Tmax for all the three curcuminoid components was observed 30 min following oral administration. AUC of nanomicellar curcuminoids was 59.2 times more than free curcuminoids. Conclusion: These data indicated that nanomicelles could improve solubility, oral bioavailability and also the stability of curcuminoids. Thus, they merit further investigation for enhancing pharmacological effects of curcuminoids.http://ijbms.mums.ac.ir/article_12252_d7c8c914cdd8434f0a317a16dc3bcb10.pdfBiological availabilityCurcuminoidDrug stabilityMicellePharmacokinetics |
| spellingShingle | Mahdi Hatamipour Amirhossein Sahebkar Seyedeh Hoda Alavizadeh Mahyar Dorri Mahmoud Reza Jaafari Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids Iranian Journal of Basic Medical Sciences Biological availability Curcuminoid Drug stability Micelle Pharmacokinetics |
| title | Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids |
| title_full | Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids |
| title_fullStr | Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids |
| title_full_unstemmed | Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids |
| title_short | Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids |
| title_sort | novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids |
| topic | Biological availability Curcuminoid Drug stability Micelle Pharmacokinetics |
| url | http://ijbms.mums.ac.ir/article_12252_d7c8c914cdd8434f0a317a16dc3bcb10.pdf |
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