Abstract
Objectives: Baclofen is a skeletal muscle relaxant with an anti-inflammatory effect. The current market products of baclofen are oral tablets and intrathecal injection which cause many undesirable systemic side effects. This study aimed to formulate topical formula of baclofen to decrease systemic side effects. Topical drug delivery systems formulated as nanoparticles (NPs) enhanced the low drug release and the low bioavailability of the traditional gels. This occurs by prolonging the contact time and increasing the permeability of the drug through the skin. Methods: In this study, formulae of the baclofen-loaded Eudragit® RL100 (ERL) NPs were prepared by nanoprecipitation method. Polyvinyl alcohol (PVA) was added as a stabilizer. The NPs were characterized by measuring their particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency percent (EE %) values. Their spherical morphology was confirmed using transmission electron microscopy (TEM). Viscosity was also measured. In vitro release and permeation studies were done to evaluate the release of the drug from the NPs gel and the permeability of the drug through the skin. The results were compared with formulated baclofen traditional gel. Results: ERL concentrationand organic phase ratio were the main factors affecting the NPs formulation. A decrease in the particle size was observed with an increase in ERL% while the smallest particle size was observed with formulae containing organic phase (acetone: methanol) in the ratio of 1: 3. The highest EE% was observed with the highest ERL concentration and the same organic phase ratio (acetone: methanol 1:3). Formulae B3, B6, B9 were selected for their most promising results. Their particle size was 187.4 ±2.81, 126.3 ±1.47, 120.0 ±1.06 nm and their EE% was 78.9 ±0.30, 83.3 ±0.26, and 86.6 ±1.12, respectively. The percentages of the drug released from the selected formulae as well as the percentage of the permeated drug were significantly higher than that of the baclofen traditional gel. Conclusion: ERL NPs were capable of releasing baclofen and improving its permeability through the skin so it may be considered as a suitable promising alternative drug delivery system.
Highlights
Skeletal muscle relaxants are used to reduce spasms and relieve pain that impairs the function of daily living activities
The UV scanning of baclofen in phosphate buffer (PB) pH 7.4 revealed that the wavelength of maximum absorbance was found to be 274 nm at pH 7.4 as shown in Figure 2.The calibration curve was constructed by plotting absorbance versus the concentration of baclofen
These three formulae were selected to study the effect of increasing Eudragit® RL100 (ERL) concentration on the morphology of NPs, the viscosity of the gel formed, the release profile, and the ex-vivo permeation studies
Summary
Skeletal muscle relaxants are used to reduce spasms and relieve pain that impairs the function of daily living activities. Baclofen is one of the oral skeletal muscle relaxants which has a narrow therapeutic index and a short biological half-life; roughly 2–4 hours[3]; in addition to the above-mentioned side effects All these obstacles encourage us to search for an alternative dosage form for baclofen. Our work aimed to formulate it as a transdermal drug delivery system (TDDS) which has many advantages over conventional modes of drug administration It avoids hepatic first-pass metabolism, enhances the bioavailability, maintains a steady plasma profile for an extended period, decreases dose frequency, improves patient compliance, enhances therapeutic efficiency, and decreases the systemic side effects produced by the oral route of skeletal muscle relaxants[4].
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