Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol (original) (raw)
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International Journal of Pharmacy and Pharmaceutical Sciences, 2016
Objective: The purpose of this study was to develop multi-unit alginate-copolymer adhesive microspheres to achieve a sustained release of terbutaline sulphate (TBS) and overcome the hepatic first pass effect so as to enhance its bioavailability. Methods: The microspheres were prepared using inotropic gelation method and different concentration of sodium alginate alone or in combination with other polymers as well as using chitosan as a coating polymer in some formulations. All of the prepared microspheres were evaluated for yield, size, encapsulation efficiency, in vitro release and mucoadhesivity. The selected formulations (F11 and F19) were further subjected to differential scanning calorimetry, Fourier transform infrared spectroscopy, stability and in vivo bioavailability studies. Results: The prepared microspheres exhibited quite widely varying encapsulation efficiencies from 20 to 74. 8 % and its mean diameter was in range of 963. 3-1. 635 µm. The in vitro release study showed a sustained release profile. The selected formulations were further subjected to differential scanning calorimetry and FTIR which confirm the absence of any incompatibility. X-ray diffraction suggests the amorphous nature of the drug after encapsulation. The selected formulation F11 and F19 showing encapsulation efficiency higher than 55 %, an amount of drug released within 50-60 % after 8 h and a relative bioavailability of 283. 84 % and 202. 04 % respectively compared with the marketed oral Aironyl ® Conclusion: The prepared microspheres were significantly efficient to achieve a sustained release of terbutaline sulphate with a higher relative bioavailability in comparison with the oral marketed tablet. tablets.
Artificial cells, nanomedicine, and biotechnology, 2018
Smart polymers such as Eudragit (ED) have shown potential applications in oral drug delivery and targeted release. Probucol (PB) is a lipophilic drug used for hypercholesterolemia and possesses desirable antidiabetic effects such as antioxidant and cell protective effects. PB is highly hydrophobic and has poor bioavailability with significant inter- and intra-patient absorption, limiting its clinical applications in diabetes. This study aimed to design and analyse new PB-ED formulations with or without the absorption-enhancer chenodeoxycholic acid (CDCA). Sodium alginate-based microcapsules containing three different ED polymers (NM30D, RL30D and RS30D) were investigated with or without CDCA via scanning electron microscopy, energy dispersive X-ray spectroscopy (EDXR), confocal microscopy, osmotic stability, mechanical properties, buoyancy, release profiles (pH: 7.4), thermal stability and antioxidant effects. The effects of microcapsules on pancreatic β-cell survival, function, inf...
FORMULATION, IN VITRO AND IN VIVO EVALUATION OF PALBOCICLIB SOLID DISPERSIONS Original Article
International Journal of Applied Pharmaceutics, 2022
Objective: The current research is aimed to enhance the dissolution and bioavailability of Palbociclib by formulating into solid dispersion Methods: The Palbociclib solid dispersions (SD) prepared by adopting different methods: Surface solid dispersion technique (SSD1-SSD15), Melt granulation (MG1-MG15) and Liquisolid compacts (LSC1-LSC9). All formulations were evaluated for physico-chemical parameters followed by in vitro dissolution studies. The optimised formulation was subjected to bioavailability studies in rats. Results: The results indicated that the prepared formulation satisfactory results for all the evaluated parameters. The SD formulations prepared by liquisolid compact and Melt Granulation technique (LSC1 and MG 3) displayed maximum dissolution of 99.64% and 99.58%. The FTIR of LSC1 displayed no interaction among drug and excipients while XRD, SEM displayed amorphous nature of drug in formulation. The stability study results indicated that LSC 1 was stable over 3 mo. The in vivo bioavailability studies conducted on rats indicate that at any time point, the drug plasma concentrations in animals administrated with the SD formulation was higher than pure drug. The Cmax of the palbociclib SD was 970.76±1.22 ng/ml and was significant (p<0.05) when compared to pure drug suspension formulation (105.84±0.19 ng/ml). The Tmax of both SD formulation and pure drug were 2.0±0.04 and 4±0.01 h, respectively. The AUC0-∞ for SD was higher 7816.61±1.37 ng. h/ml) than the pure drug suspension 2501.4±1.46 ng. h/ml indicating better systemic drug absorption from SD formulation prepared using Melt granulation technique. Conclusion: A significant enhancement in vitro dissolution profile and bioavailability of the melt granules was observed compared to the pure Palbocicilib and marketed product.
2017
The goal of any ideal drug delivery system is to provide a therapeutic amount of drug to the proper site in the body to achieve prompt response, and thus maintain the desired drug concentration. Such a conceptualized ideal drug delivery can be possible with intravenous infusion of drug at the site of action over a desired period of time. The aim of this study to different marketed product which is use in various drug delivery systems like Controlled release drug delivery and Transdermal drug delivery, the colon is a site where both local and systemic delivery of drugs can take place. Local delivery allows topical treatment of inflammatory bowel disease. However, treatment can be made effective if the drugs can be targeted directly into the colon, thereby reducing the systemic side effects. Controlled release dosage forms cover a wide range of prolonged action formulations, which provide continuous release of their active ingredients at a predetermined rate and time. The majority of ...
Diabetes, Obesity and Metabolism, 2020
AimTo evaluate the efficacy and safety of polyethylene glycol loxenatide (PEX168) monotherapy in type 2 diabetes (T2D) patients in China.Materials and MethodsIn a multicentred, randomized, double‐blinded, placebo‐controlled phase 3a clinical trial, 361 patients with inadequate glycaemic control (HbA1c 7.0%‐10.5%, fasting plasma glucose <13.9 mmol/L) were randomized (1:1:1) for weekly subcutaneous injections: placebo, PEX168/100 μg or PEX168/200 μg. The 24‐week treatment was followed by a 28‐week extension, during which placebo‐treated patients were randomly assigned to PEX168/100 μg or PEX168/200 μg. The primary efficacy endpoint was the HbA1c change from baseline to week 24.ResultsThe three groups had similar demographics and baseline characteristics. The HbA1c least‐square mean (95% CI) change from baseline to week 24 was greater for PEX168/100 μg (−1.02% [−1.21%, −0.83%]) and PEX168/200 μg (−1.34% [−1.54%, −1.15%]) than for placebo (−0.17% [−0.36%, 0.02%]); (superiority: P <...
Materials Science and Engineering: C, 2009
Poly-(3-hydroxybutyrate) (P(3HB)) is a biodegradable and biocompatible polymer that has been used to obtain polymer-based drug carriers. However, due to the high crystallinity degree of this polymer, drug release from P(3HB) microspheres frequently occurs at excessive rates. In this study, two strategies for prolonging ibuprofen release from P(3HB)-based microspheres were tested: blending with poly(D,L-lactide)-b-polyethylene glycol (mPEG-PLA); and obtaining composite particles with gelatin (GEL). SEM micrographs showed particles that were spherical and had a rough surface. A slight decrease of the crystallinity degree of P(3HB) was observed only in the DSC thermogram obtained from unloaded-microspheres prepared from 1:1 P(3HB):mPEG-PLA blend. For IBF-loaded microspheres, a reduction of around 10 °C in the melting temperature of P(3HB) was observed, indicating that the crystalline structure of the polymer was affected in the presence of the drug. DSC studies also yielded evidence of the presence of a molecular dispersion coexisting with a crystalline dispersion in the drug in the matrix. Similar results were obtained from X-ray diffractograms. In spite of 1:1 mPEG-PLA:P(3HB) blends having contributed to the reduction of the burst effect, a more controlled drug release was provided by the use of the 3:1 P(3HB):mPEGPLA blend. This result indicated that particle hydration played an important role in the drug release. On the other hand, the preparation of P(3HB):GEL composite microspheres did not allow control of the IBF release.