Abstract

Objectives: The primary objective of the present study is to develop and evaluate tizanidine hydrochloride (TZ) solid lipid nanoparticles (SLNs) using solid lipids/triglycerides.
 Methods: TZ SLNs were prepared by hot homogenization followed by ultrasonication technique. The prepared SLNs were characterized for drug content, entrapment and loading efficiency, particle size, zeta potential, polydispersity index (PDI), and in intro release kinetics.
 Results: TZ SLNs were prepared. The particle size ranged from 49.7 to 523.7 nm. PDI of all formulations was good within the range of 0.189–0.487. The zeta potential of blank SLNs was −15.2 mV whereas drug-loaded SLNs showed zeta potential from −8.85 mV to −42.0 mV. Entrapment efficiency observed was in the range of 34.5–75.0%. The cumulative percentage release of TZ from different TZ nanoparticles varied from 35.28% to 83.98% depending on the drug-lipid ratio and the type of lipid and surfactant used. The release kinetic studies of optimized formulation showed that the release was first order and the release mechanism was non-Fickian type.
 Conclusion: The prepared SLNs were able to sustain the drug release for 24 h, thus reducing dosing frequency and occurrence of side effects, thereby increasing the effectiveness of the drug.

Highlights

  • Most of the people prefer oral route of administration as the major route of administration of pharmaceuticals having the advantage of being painfree, convenient to handle, and noninvasive [1]

  • We aim to develop tizanidine hydrochloride (TZ) loaded Solid lipid nanoparticles (SLNs), which sustains the drug release thereby increasing the efficiency of the treatment

  • Preformulation studies Drug-polymer interaction study by Fourier-transform infrared spectroscopy (FTIR) spectrophotometer The FTIR was performed for the drug (TZ), lipids (CM, TS, and Glyceryl monostearate (GMS)), and physical mixture of drug and lipids (TZ and Compritol 888 (CM), TZ and TS, and TZ and GMS)

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Summary

Introduction

Most of the people prefer oral route of administration as the major route of administration of pharmaceuticals having the advantage of being painfree, convenient to handle, and noninvasive [1]. The oral dosage form has several disadvantages. To overcome the disadvantages of the oral route of administration, many new powerful drug substances have been found due to new technologies employed in drug discovery. Solid lipid nanoparticles (SLNs) are the novel drug delivery system in which the active drug is incorporated into lipid carriers with the help of the stabilizers. They are solid colloids having the size in nanometers that range from 10 to 1000 nm at least in one dimension (generally 50–500 nm) [2]. SLNs combine the advantages of and simultaneously avoid the limitations of polymeric nanoparticles, fat emulsions, and liposomes [3]

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