Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .
Background: Bilosomes are vesicular nanocarriers that contain bile salts, making them more flexible and resistant to degradation in the gastrointestinal tract. Objective: To evaluate the effect of two bile salts on the physical properties and stability of the ropinirole-loading bilosome. Methods: Sixteen bilosomal formulations were prepared by a reverse-phase evaporation method. Each formula includes a mixture of non-ionic surfactants (Span®60 and Tween®60), along with cholesterol and bile salts (either sodium taurocholate (STC) or sodium glycocholate (SGC). The characteristics of the bilosomal formulations (drug content, entrapment efficiency, vesicle size, polydispersity index, zeta potential, in-vitro drug release, and Fourier transform infrared spectroscopy) were evaluated. Results: The entrapment efficiency of ropinirole was reduced by using sodium glycocholate instead of sodium taurocholate. The vesicle size and zeta potential were also affected by the type of bile salt and its amount. Drug release profiles were sustained, indicating a good entrapment of ropinirole. The STC-containing bilosomes are more stable than the SGC-containing bilosomes. Bilosomal formula F5 showed the highest entrapment efficiency (64.82%), suitable vesicle size (179.8 nm), zeta potential (-9.162 mV), polydispersity index (0.5116), and in vitro drug release (62.33%) after 24 hr. Conclusion: Sodium taurocholate was more suitable for the preparation of ropinirole-loading bilosomes, with more stability of bilosomes in bile salt solution.
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