Agglomerated Oral Dosage Forms of Artemisinin/β-Cyclodextrin Spray-Dried Primary Microparticles Showing Increased Dissolution Rate and Bioavailability

Context: Ever since the discovery of cyclodextrins, a family of cyclic oligosaccharides based on a (1 ! 4) linkage among glucopyranose subunits, these versatile supramolecular hosts have received tremendous attention for scientific explorations. Due to their property of forming host-guest type inclusion complex, cyclodextrins and their synthetic derivatives exhibit wide range of utilities in different areas viz. pharmaceuticals, drug delivery systems, cosmetics, food and nutrition, textile and chemical industry etc. Objective: The purpose of this review is to highlight properties, advantages, recent studies and versatile benefits of cyclodextrins and to re-strengthen their prospective applications in novel directions for future research. Methods: This article summarizes a variety of applications of cyclodextrins in various industrial products, technologies, analytical and chemical processes and recent industrial advancements by extensively literature search on various scientific databases, Google and websites of various associated pharmaceutical industries and patenting authorities across the world. Results and conclusion: Due to possibility of multidimensional changes in physical and chemical properties of molecules upon inclusion complexation in cyclodextrins, these compounds are of great commercial interest and may offer solution to many of the scientific problems of the current world.

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“…Balducci et al (2013) Norfloxacin b-CD The solid-state properties of complexes of b-CD and norfloxacin at the molecular level.…”

Section: Cds In Bioconversion Processmentioning

confidence: 99%

Exploring versatile applications of cyclodextrins: an overview

2014

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“…30, 35 In comparison, oral delivery route resulted in longer T max . 29 In all these studies, the half-life of artemisinin is short (~30 min in rats, ~2 h in humans), 31, 32 which might be due to rapid metabolism and elimination by the liver and to a lesser extent by other organs such as lungs and kidneys. 36 In human, artemisinin is metabolized in the liver by cytochrome P450s including CYP2B6 and CYP3A4, 37 yielding a number of metabolites that are excreted in urine, 38 while urinary excretion of unchanged artemisinin is negligible 31 .…”

Section: Discussionmentioning

confidence: 99%

Development of a Specific Monoclonal Antibody for the Quantification of Artemisinin in Artemisia annua and Rat Serum

et al. 2016

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Artemisinin, extracted from Artemisia annua, and its derivatives are important frontline antimalarials. To produce specific antibodies for the detection and quantification of artemisinin, artemisinin was transformed to 9-hydroxyartemisinin by microbial fermentation, which was used to prepare a 9-succinate artemisinin hapten for conjugation with ovalbumin. A monoclonal antibody (mAb), designated as 3H7A10, was selected from hybridoma cell lines which showed high specificity to artemisinin. No competitive inhibition was observed with artesunate, dihydroartemisinin, and artemether for up to 20,000 ng mL−1. An indirect competitive enzyme-linked immunosorbent assay (icELISA) was developed, which showed a concentration causing 50% of inhibition (IC50) for artemisinin as 2.6 ng mL−1 and a working range of 0.6–11.5 ng mL−1. The icELISA was applied for the quantification of artemisinin in crude extracts of wild A. annua and the study of pharmacokinetics of artemisinin in rat serum after intraperitoneal injection. The results were highly correlated with those determined by HPLC-UV analysis (R2=0.9919). In comparison with reported anti-artemisinin mAbs which have broad cross reactivity with other artemisinin derivatives, the high specificity of 3H7A10 for artemisinin will enable development of methods for quantification of artemisinin in Artemisia plants and antimalarial drugs such as Arco®, and for pharmacokinetic studies.

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“…Although other strategies to optimise artemisinin drug delivery have been investigated [18], one of the potentially promising strategies is the use of nanomedicine drug delivery systems (NMDDS) which exhibit exceptional characteristics such as target specificity, increased solubility, protection from acid degradation, and a large surface to volume ratio which allows drugs to penetrate through cell and tissue barriers [19, 20]. …”

Section: Introductionmentioning

confidence: 99%

Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method

Masiiwa

Gadaga

2018

Journal of Drug Delivery

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Background Artesunate is one of the most potent, rapidly acting and therapeutically versatile antimalarial drugs. Its efficacy is hampered by poor aqueous solubility and stability resulting in low oral bioavailability. Recent efforts to nanoformulate artesunate have shown great potential of improving its dissolution profile and bioavailability. However, no study has yet been done to investigate the intestinal permeability of these nanoformulations, which is a critical determinant of systemic absorption. Objective of the Study The main aim of the study was to determine the intestinal permeability of artesunate-loaded solid lipid nanoparticles (SLN). Method The microemulsion dilution technique was used to fabricate artesunate-loaded solid lipid nanoparticles. In vitro drug release studies were performed at pH 1.2 and 6.8 using the dialysis membrane method. The everted gut sac method was used to assess the intestinal permeability of the prepared nanoparticles. Results The average particle size was 1109 nm and the polydispersity index (PDI) was 0.082. The zeta potential was found to be −20.7 mV. The encapsulation efficiency of the solid lipid nanoparticles obtained was 51.7%. At both pH 1.2 and 6.8, pure artesunate was rapidly released within the first 30 mins while the SLN showed a biphasic release pattern with an initial burst release during the first hour followed by a prolonged release over time. The rate of drug release increased with increasing pH. The apparent permeability (Papp) of SLN was found to be greater (0.169 mg/cm2) as compared to that of pure artesunate (0.117 mg/cm2) at the end of the experiment. Conclusion The results obtained in this study showed that the microemulsion dilution technique can be used to formulate artesunate solid lipid nanoparticles. The formulation exhibited a sustained drug release profile. The intestinal permeability of artesunate could be enhanced by the nanoformulation.

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Agglomerated Oral Dosage Forms of Artemisinin/β-Cyclodextrin Spray-Dried Primary Microparticles Showing Increased Dissolution Rate and Bioavailability

Cited by 25 publications

References 23 publications

Exploring versatile applications of cyclodextrins: an overview

Exploring versatile applications of cyclodextrins: an overview

Development of a Specific Monoclonal Antibody for the Quantification of Artemisinin in Artemisia annua and Rat Serum

Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method

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