Volume 15, Issue 2 (Summer 2023)
2023, 15(2): 1-12 |
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Ethics code: IR.MUMS.PHARMACY.REC.1397.098
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Kamali H, Khodaverdi E, Jafarzadeh N, Rezaeian Shiadeh S N, Hadizadeh F. Sustained Release In-situ Forming Liquid Crystal Gel Containing Risperidone: In-vitro Evaluation and Pharmacokinetics in Rabbits. North Khorasan University of Medical Sciences 2023; 15 (2) :1-12
URL: http://journal.nkums.ac.ir/article-1-2785-en.html
URL: http://journal.nkums.ac.ir/article-1-2785-en.html
Hossein Kamali1 
, Elham Khodaverdi2 , Nazanin Jafarzadeh3 , Seyedeh Nesa Rezaeian Shiadeh4 , Farzin Hadizadeh *5
, Elham Khodaverdi2 , Nazanin Jafarzadeh3 , Seyedeh Nesa Rezaeian Shiadeh4 , Farzin Hadizadeh *5
1- Assistant Professor, Ph.D. in Pharmaceutics, Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran
2- Professor, Ph.D. in Pharmaceutics, Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
3- Student, Pharm.D, Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
4- Assistant Professor, Ph.D. in Pharmaceutics, Department of Pharmaceutics, School of Pharmacy, Hormozgan University of Medical Sciences, Bandar abbas, Iran
5- Professor, Ph.D. in Medicinal Chemistry, Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
2- Professor, Ph.D. in Pharmaceutics, Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
3- Student, Pharm.D, Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
4- Assistant Professor, Ph.D. in Pharmaceutics, Department of Pharmaceutics, School of Pharmacy, Hormozgan University of Medical Sciences, Bandar abbas, Iran
5- Professor, Ph.D. in Medicinal Chemistry, Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
Abstract: (1331 Views)
Introduction: The present study aimed to extend a novel vehicle for sustained delivery of risperidone to improve schizophrenia therapy. Risperidone is used as an anti-psychotic drug to treat various psychological conditions. Lipid liquid crystal (LLC) gel containing various lipids, solvents, and stabilizers turns into a sustain-release gel in contact with the aqueous medium.
Method: Glycerol monooleate (GMO), glycerol dioleate (GDO), and glycerol trioleate (GTO) alongside several ratios of phosphatidylcholine (PC) to oil and N-methyl-2-pyrrolidone (NMP) solvent percent (w/w %) were assessed for initial burst release (IBR) for LLC. Some In-vitro evaluations, pharmacokinetics assessments, and histopathological studies were done to gain optimal formulation.
Results: the GDO-based LLC showed lower IBR in comparison to other glycerol-based formulations. Pharmacokinetic data revealed that GDO at PC:oil = 2.2:1 and NMP = 30% made a sustained release for two months. Risperdal CONSTA® can reach the required therapeutic levels after 2–3 weeks; however, over the lag period, co-administration of oral risperidone is essential. The histopathology results indicated approximately no side effects in rabbits.
Conclusion: This study confirms the great potential of GDO-based LLC in comparison to Risperdal CONSTA®. Furthermore, the results showed that a single injection of GDO-based formulations could maintain drug release in both in-vitro and in-vivo for two months in the therapeutic range.
Method: Glycerol monooleate (GMO), glycerol dioleate (GDO), and glycerol trioleate (GTO) alongside several ratios of phosphatidylcholine (PC) to oil and N-methyl-2-pyrrolidone (NMP) solvent percent (w/w %) were assessed for initial burst release (IBR) for LLC. Some In-vitro evaluations, pharmacokinetics assessments, and histopathological studies were done to gain optimal formulation.
Results: the GDO-based LLC showed lower IBR in comparison to other glycerol-based formulations. Pharmacokinetic data revealed that GDO at PC:oil = 2.2:1 and NMP = 30% made a sustained release for two months. Risperdal CONSTA® can reach the required therapeutic levels after 2–3 weeks; however, over the lag period, co-administration of oral risperidone is essential. The histopathology results indicated approximately no side effects in rabbits.
Conclusion: This study confirms the great potential of GDO-based LLC in comparison to Risperdal CONSTA®. Furthermore, the results showed that a single injection of GDO-based formulations could maintain drug release in both in-vitro and in-vivo for two months in the therapeutic range.
Keywords: Lipid liquid crystal, Risperidone, Glycerol mono-oleate, Glycerol-dioleate, Glycerol-trioleate
Type of Study: Orginal Research |
Subject:
Basic Sciences
Received: 2022/01/29 | Accepted: 2023/03/4 | Published: 2023/08/26
Received: 2022/01/29 | Accepted: 2023/03/4 | Published: 2023/08/26
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