| 1. |
- AlHayali, Amani, et al.
(författare)
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Silodosin oral films : Development, physico-mechanical properties and in vitro dissolution studies in simulated saliva
- 2019
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 53
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Tidskriftsartikel (refereegranskat)abstract
- Sublingual film dosage forms for drugs used for fast symptomatic treatment have promise because they allow a rapid onset of action. The aim of this study was to prepare films of silodosin intended for sublingual administration for the symptomatic treatment of benign prostatic hyperplasia in men. Hydroxypropyl methylcellulose (HPMC) or hydroxypropyl methylcellulose acetate succinate (HPMC-AS) were used as film-forming polymers. The effects of the polymers and the surfactant tocopherol polyethylene glycol succinate (TPGS) on the physico-mechanical properties and dissolution behavior of the films in simulated saliva were investigated. The eight silodosin oral films developed (F1–F8) contained 8 mg silodosin per 6 cm2 film and HPMC or HPMC-AS in drug:polymer ratios of 1:5 or 1:3, while four also contained TPGS (0.5% w/w). The films were characterized using DSC, TGA, SEM, and PXRD and the mechanical properties were investigated by measuring tensile strength, elongation at break and Young's modulus. The mechanical properties of the films were dependent on the ratio of polymer used. The in vitro dissolution and drug release studies indicated that HPMC-AS films disintegrated more quickly than HPMC films. Silodosin was shown to be dispersed within the polymers. Despite silodosin being submicronized in the HPMC films, the dissolution and drug release rate (time for 80% release) from HPMC films was significantly faster than from HPMC-AS films. TPGS increased the drug release rate to a greater extent with HPMC than with HPMC-AS. The degree of saturation of formulation F4 was >1, which shows potential for improving oral absorption of silodosin.
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| 2. |
- Alomari, Mustafa, et al.
(författare)
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Printing of T3 and T4 Oral Drug Combinations as a Novel Strategy for Hypothyroidism
- 2018
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Ingår i: International Journal of Pharmaceutics. - : Elsevier. - 0378-5173 .- 1873-3476. ; 549:1-2, s. 363-369
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Tidskriftsartikel (refereegranskat)abstract
- Hypothyroidism is a chronic and debilitating disease that is estimated to affect 3% of the general population. Clinical experience has highlighted the synergistic value of combining triiodothyronine (T3) and thyroxine (T4) for persistent or recurrent symptoms. However, thus far a platform that enables the simultaneous and independent dosing of more than one drug for oral administration has not been developed. Thermal inkjet (TIJ) printing is a potential solution to enable the dual deposition of T3 and T4 onto orodispersible films (ODFs) for therapy personalisation. In this study, a two-cartridge TIJ printer was modified such that it could print separate solutions of T3 and T4. Dose adjustments were achieved by printing solutions adjacent to each other, enabling therapeutic T3 (15–50 μg) and T4 dosages (60–180 μg) to be successfully printed. Excellent linearity was observed between the theoretical and measured dose for both T3 and T4 (R2 = 0.982 and 0.985, respectively) by changing the length of the print objective (Y-value). Rapid disintegration of the ODFs was achieved (< 45 seconds). As such, this study for the first time demonstrates the ability to produce personalised dose combinations by TIJ printing T3 and T4 onto the same substrate for oral administration.
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| 3. |
- Chakraborty, Subhashis, et al.
(författare)
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Effective in-vivo utilization of lipid-based nanoparticles as drug carrier for carvedilol phosphate
- 2011
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Ingår i: Journal of Pharmacy and Pharmacology (JPP). - : Oxford University Press (OUP). - 0022-3573 .- 2042-7158. ; 63:6, s. 774-779
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Tidskriftsartikel (refereegranskat)abstract
- Objectives Lipid nanoparticles as carrier for oral drug administration improve gastrointestinal solubility of poorly soluble drugs and thus enhance bioavailability. However, basic drugs may undergo rapid dissolution from such solid dispersions in the stomach and precipitate in the intestine due to their higher solubility in acidic medium. Therefore, the objective of this work was to study the enhancement in bioavailability of carvedilol phosphate (basic drug) by providing an alkaline gastric environment to drug-loaded solid lipid nanoparticles. Methods An alkaline gastric environment in rats was created and maintained with oral administration of an antacid suspension 5 min before and 30 min post dosing. Key findings The formulation administered orally exhibited enhanced bioavailability (∼27%) when compared with drug suspension and sustained release behaviour when compared with formulation under ideal gastric conditions. The enhanced bioavailability is due to the presence of lipid nanoparticles as drug carrier while the sustained-release characteristic may be attributed to the presence of antacid, which resulted in elevation of gastric pH and reduced the drug's solubility. Conclusions It may be concluded that although lipid nanoparticles can be instrumental in improving bioavailability, additional sustained release may be achieved by targeting intestinal release of basic drugs from lipid vehicles, which is possible by incorporating them into suitable enteric-coated formulations.
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| 4. |
- Chakraborty, Subhashis, et al.
(författare)
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Utilization of adsorption technique in the development of oral delivery system of lipid based nanoparticles
- 2010
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Ingår i: Colloids and Surfaces B. - : Elsevier BV. - 0927-7765 .- 1873-4367. ; 81:2, s. 563-569
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Tidskriftsartikel (refereegranskat)abstract
- The objective of the present study was to employ suitable adsorbent with free flowing characteristics for improving the stability and physical properties of solid lipid nanoparticles (SLN) for oral administration. Stearic acid based nanoparticles of carvedilol phosphate were fabricated by solvent emulsification evaporation technique in sodium taurocholate solution prepared in pH 7.2 buffers (I-KH2PO4/NaOH or II-NaH2PO4/Na2HPO4) with 1% polyvinyl alcohol. Nanoparticles were then adsorbed by passing the nanodispersion through a Neusilin US2 (adsorbent) column. Interestingly, scanning electron microscopy revealed round deformed and even collapsed nanoparticles in Buffer-I and discrete spherical to ellipsoidal nanoparticles in Buffer-II which indicates the inability of nanoemulsion to crystallize and form SLN in Buffer-I. The successful formation of SLN in Buffer-II was confirmed by differential scanning calorimetry and X-ray diffraction. The retention of SLN from the nanodispersion by adsorption on the adsorbent imparted good flow property and resulted in a marked stability improvement of the formulation in terms of drug retention efficiency and release profile as compared to the simple nanosuspension. In conclusion, the adsorbent technology would be instrumental in imparting additional features to the existing conventional colloidal system for pharmaceutical application which would ease the process of capsule filling at industrial scale, simplify the handling of formulations by patients and can significantly improve the shelf life of the product for a longer period of time as compared to liquid formulations
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| 5. |
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| 6. |
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| 7. |
- Kushwaha, Anand Kumar, et al.
(författare)
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Development and evaluation of solid lipid nanoparticles of raloxifene hydrochloride for enhanced bioavailability
- 2013
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Ingår i: BioMed Research International. - : Hindawi Limited. - 2314-6133 .- 2314-6141. ; 2013
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Tidskriftsartikel (refereegranskat)abstract
- Raloxifene hydrochloride (RL-HCL) is an orally selective estrogen receptor modulator (SERM) with poor bioavailability of nearly 2% due to its poor aqueous solubility and extensive first pass metabolism. In order to improve the oral bioavailability of raloxifene, raloxifene loaded solid lipid nanoparticles (SLN) have been developed using Compritol 888 ATO as lipid carrier and Pluronic F68 as surfactant. Raloxifene loaded SLN were prepared by solvent emulsification/evaporation method, and different concentrations of surfactant, and homogenization speed were taken as process variables for optimization. SLN were characterized for particle size, zeta potential, entrapment efficiency, surface morphology, and crystallinity of lipid and drug.In vitrodrug release studies were performed in phosphate buffer of pH 6.8 using dialysis bag diffusion technique. Particle sizes of all the formulations were in the range of 250 to 1406 nm, and the entrapment efficiency ranges from 55 to 66%. FTIR and DSC studies indicated no interaction between drug and lipid, and the XRD spectrum showed that RL-HCL is in amorphous form in the formulation.In vitrorelease profiles were biphasic in nature and followed Higuchi model of release kinetics. Pharmacokinetics of raloxifene loaded solid lipid nanoparticles after oral administration to Wistar rats was studied. Bioavailability of RL-HCL loaded SLN was nearly five times than that of pure RL-HCL.
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| 8. |
- Mishra, Amit, et al.
(författare)
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Intestinal Lymphatic Delivery of Praziquantel by Solid Lipid Nanoparticles: Formulation Design, In Vitro and In Vivo Studies
- 2014
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Ingår i: Hans Journal of Nanotechnology. - : Hindawi Limited. - 2161-086X .- 2161-0878 .- 1687-9503 .- 1687-9511. ; 2014
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Tidskriftsartikel (refereegranskat)abstract
- The aim of the present work was to design and develop Praziquantal (PZQ) loaded solid lipid nanoparticles (PZQ-SLN) to improve the oral bioavailability by targeting intestinal lymphatic system. PZQ is practically insoluble in water and exhibits extensive hepatic first-pass metabolism. PZQ SLN were composed of triglycerides, lecithin and various aqueous surfactants; were optimized using hot homogenization followed by ultrasonication method. The optimized SLN had particle size of 123 ± 3.41 nm, EE of 86.6 ± 5.72 %. The drug release of PZQ-SLN showed initial burst release followed by the sustained release. Inspite of zeta potential being around -10 mV, the optimized SLN were stable at storage conditions (5 ± 3 °C and 25 ± 2°C/ 60 ± 5 % RH) for six months. TEM study confirmed the almost spherical shape similar to the control formulations. Solid state characterization using differential scanning calorimeter (DSC) and powder X-ray diffraction (PXRD) analysis confirmed the homogeneous distribution of PZQ within the lipid matrix. The 5.81-fold increase in AUC 0 → ∞, after intraduodenal administration of PZQ-SLN in rats treated with saline in comparison to rats treated with cycloheximide (a blocker of intestinal lymphatic pathway), confirmed its intestinal lymphatic delivery. The experimental results indicate that SLN may offer a promising strategy for improving the therapeutic efficacy and reducing the dose.
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| 9. |
- Montenegro-Nicolin, Miguel, et al.
(författare)
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The Effect of Inkjet Printing over Polymeric Films as Potential Buccal Biologics Delivery Systems
- 2018
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Ingår i: AAPS PharmSciTech. - : Springer. - 1530-9932. ; 19:8, s. 3376-3387
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Tidskriftsartikel (refereegranskat)abstract
- The buccal mucosa appears as a promissory route for biologic drug administration, and pharmaceutical films are flexible dosage forms that can be used in the buccal mucosa as drug delivery systems for either a local or systemic effect. Recently, thin films have been used as printing substrates to manufacture these dosage forms by inkjet printing. As such, it is necessary to investigate the effects of printing biologics on films as substrates in terms of their physical and mucoadhesive properties. Here, we explored solvent casting as a conventional method with two biocompatible polymers, hydroxypropyl methylcellulose, and chitosan, and we used electrospinning process as an electrospun film fabrication of polycaprolactone fibers due to its potential to elicit mucoadhesion. Lysozyme was used as biologic drug model and was formulated as a solution for printing by thermal inkjet printing. Films were characterized before and after printing by mechanical and mucoadhesive properties, surface, and ultrastructure morphology through scanning electron microscopy and solid state properties by thermal analysis. Although minor differences were detected in micrographs and thermograms in all polymeric films tested, neither mechanical nor mucoadhesive properties were affected by these differences. Thus, biologic drug printing on films was successful without affecting their mechanical or mucoadhesive properties. These results open way to explore biologics loading on buccal films by inkjet printing, and future efforts will include further in vitro and in vivo evaluations.
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| 10. |
- Purvin, Shah, et al.
(författare)
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Pharmacokinetic and tissue distribution study of solid lipid nanoparticles of zidovudine in rats
- 2014
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Ingår i: Journal of Nanotechnology. - : Hindawi Limited. - 1687-9503 .- 1687-9511. ; 2014
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Tidskriftsartikel (refereegranskat)abstract
- Zidovudine-loaded solid lipid nanoparticles (AZT-SLNs) and zidovudine in solution were prepared and administered in rats. The aim of this research was to study whether the bioavailability of zidovudine can be improved by AZT-SLNs perorally to rats as compared to oral administration of zidovudine. Zidovudine was determined in plasma and tissues by reverse phase high performance liquid chromatography. The pharmacokinetic parameters of zidovudine were determined after peroral administration: area under curve of concentration versus time (AUC) for AZT-SLNs was 31.25% greater than AZT solution; meanwhile mean resident time (MRT) was found to be 1.83 times higher for AZT-SLNs than AZT solution. Elimination half life of zidovudine was also increased for SLN formulation. Tissue distribution pattern of zidovudine was changed in case of AZT-SLNs. AUC of zidovudine in brain and liver was found to be approximately 2.73 and 1.77 times higher in AZT-SLNs than AZT solution, respectively, indicating that AZT-SLNs could cross blood brain barrier. Distribution of zidovudine was approximately 0.95 and 0.86 times lesser in heart and kidney, respectively. It can be concluded from the study that oral administration of AZT-SLNs modifies the plasma pharmacokinetic parameters and biodistribution of zidovudine.
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