Migraine is the second most common neurological illness, aff ecting around one billion people each year; triptans are commonly used in the treatment; rizatriptan benzoate is a member of the triptan class, it’s available as a tablet dosage form. Unfortunately, it undergoes fi rst-pass eff ect after oral intake. The intranasal route of administration represents a solve to such a problem. Because it has a limited permeability, an eff ort has been made to circumvent this hurdle. Nanotechnology’s innovation has off ered a useful answer to several issues in the pharmaceutical fi eld in which it could improve drug permeability. The aim of the present work involved loading rizatriptan benzoate on a nanostructured lipid carrier as an attempt to resolve adversity affi liated with the intended drug. The high-speed homogenization technique prepares six formulas. The formulations’ particle size, polydispersity index, zeta potential, entrapment effi ciency, loading capacity, and in-vitro drug release were studied. Diff erential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and powder X-ray diff raction (PXRD) was investigated to exclude drug excipient incompatibility and to evaluate the crystallinity state of rizatriptan benzoate before and after formulation. Successful formulations were obtained with an acceptable nanostructured parameter In-vitro drug release profi le illustrates a biphasic pattern in which an immediate followed by a persistent phase over a 6 hours. release period, with an estimated percent of the medication being released with an anomalous release mechanism. The compatibility and crystallinity investigation revealed that rizatriptan benzoate was compatible with the other excipients used in the research, and the drug molecule was found to be in an amorphous state within the lipid matrix. In conclusion, nanostructured lipid carriers might be a potential delivery approach for improving intranasal administration of rizatriptan benzoate.
Nanotechnology represents a magic wand to solve most problems related to improving drug effi ciency, one of the most important of these problems is the drug’s permeability through biological membranes. Rizatriptan benzoate was used for the treatment of acute migraine, it has poor permeability and is diffi cult to administer through the nose. This study aims to design a nanostructured lipid carrier containing rizatriptan benzoate as a trial to enhance its biological permeability. A high shear homogenization technique was utilized as a method of preparation; glyceryl monostearate and becs wax are used as solid lipids while oleic acid and castor oil were used as liquid lipids in diff erent ratios. Particle size analysis, polydispersity index, zeta potential, entrapment effi ciency, and loading effi ciency were considered the main criteria for the evaluation, meanwhile, the in-vitro release test was done for the formulas having smallest particle size. Moreover, the infrared spectroscopy and diff erential scanning calorimetry (DSC) are investigated for the selected formula. The obtained outcome revealed a signifi cant eff ect on the particle size and entrapment effi ciency upon enhancing the ratio of liquid lipid. Furthermore, changing the type of solid and liquid lipid leads to a dramatic alteration in the criteria of evaluation, also biphasic release pattern was seen. The infrared spectroscopy shows an intact rizatriptan benzoate, while DSC revealed a change of drug molecule to an amorphous state. In conclusion, a high shear homogenization can be used to formulate a successful nanostructured lipid carrier with good physical properties.
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