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Despite the noticeable advantages of the liposomes and polymersomes, they also revealed some drawbacks that could be minimized by preparing hybrid vesicular systems and integrating the advantage of both vehicles into one system named lipopolymersome. Lipopolymesome incorporates the biodegradability, stability, adjustability and chemical flexibility of polymersomes with the elasticity, soft nature and biocompatibility of liposomes. In the current study, wereported the development of five nanoscale lipopolymersomal hybrid vesicular systems consisting different molar ratios of dipalmitoylphosphatidylcholine (DPPC) and poly (ethylene glycol)-poly (lactic acid) (PEG-PLA) (PEG-PLA DPPC ratio of 1000, 5050 2575, 7525 and 0100). Rhod-6G-loaded hybrid vesicles were prepared via film rehydration. Then, the efficacy of five formulations were evaluated in terms of loading capacity, release pattern, cellular uptake, andin vivobiodistribution in ectopic tumor model in mice. The obtained results demonstrated that the self-assembly, loading capacity, cargo release and stability of hybrid nanoscale lipopolymersomes can be tuned by incorporation of amphiphilic lipid-polymers at various ratios. In this regard, the prepared hybrid nanovesicles consisting of DPPC-PEG-PLA (2575) exhibited great potential through superior loading capacity, stability and tumor accumulation compared with other systems. It could be concluded that the prepared lipopolymersome offers important opportunities for the development of novel hybrid carriers for efficient transportation of therapeutics into tumor site.Minimization of radiation coming from the chamber wall during lyophilization has the potential to reduce the edge-vial-effect. The edge-vial-effect is a phenomenon in which vials positioned at the shelf edges and corners tend to run warmer compared to center vials. A higher product temperature may result in product collapse in these vials. this website Consequently, more conservative and time-consuming freeze-drying cycles with lower shelf temperatures and pressures are chosen to ensure a product temperature below the collapse temperature in all vials. The edge-vial-effect is of even higher impact in small batches, where the ratio of corner and edge to center vials is higher compared to large scale manufacturing. The chamber wall is often discussed as the primary source of radiation impacting corner and edge vials. A radiation cage was set at different low temperatures to determine the impact of chamber wall temperatures below 0 °C on product temperature. At the end of primary drying, product temperature of corner vials could be reduced by 6 °C through the radiation cage but primary drying was elongated. Compared to vials in a tray, the chamber wall temperature had less impact on vials nested in a rack system due to a shielding effect of the rack itself. Corner and center vials ran more homogeneous with radiation cage since the edge and corner vials were slowed down. The difference in primary drying time between corner and center vials in the tray could be significantly reduced by 18% by means of 7 h when the radiation cage was controlled at product temperature and combined with a higher shelf temperature. In summary, the radiation cage is a useful tool for a more homogeneous batch with the potential to reduce primary drying time. Nevertheless, the drying difference between corner and center vials could only be reduced and was not completely eliminated.Low-frequency Raman (LFR) spectroscopy probes vibrational modes related to long-range order (i.e., crystallinity) that can provide unique information on the solid-state/structural characteristics among other properties. Furthermore, the recent advancements in instrumentation (most notably, narrow wavelength band filters) and data analysis has allowed to overcome some of the previous limitations of this technique. In fact, LFR spectroscopy has now enjoyed a surge in popularity with applications found in many research areas. This mini-review article provides a comprehensive summary of established and exciting new LFR applications for pharmaceutical analysis. Aspects of the underlying theory, instrumentation and data analysis (including application of chemometric and computational techniques) are also discussed in detail.The aim of this study was to resolve the lag time problem for peptides loaded PLGA-Hydrogel Microspheres (PLGA-gel-Ms) by blending low molecular PLGA (Mw. 1 kDa) into PLGA (Mw. 10 kDa) as an intrinsic porogen, and then assess the in vitro-in vivo relationship (IVIVR). Here, Goserelin acetate (GOS) was chosen as the model peptides. When compared to additional types of porogen, the intrinsic porogen avoided impurities remaining and protected the bioactivities of the peptides. By adding 10% PLGA (Mw. 1 kDa), the lag time was eliminated both in vitro and in vivo with a desirable EE (97.04% ± 0.51%). The release mechanisms were found to be a) initial GOS release mainly controlled by pores diffusion and b) autocatalysis of PLGA (Mw. 1 kDa) which increased the quantity of aqueous pores, as revealed by SEM images. To solve the challenges caused by multiphasic release profiles, for the first time the Segmented phases IVIVR were proposed and developed, and showed improved linear fitting effects and supported the proposed release mechanisms. The application of PLGA blends could provide a new insight into PLGA microsphere initial release rate regulation.A diverse set of drug and polymer combinations have been effectively evaluated utilizing a newly developed method called acoustic fusion to form amorphous solid dispersions (ASD) on the mg-scale, indicating that this approach is a general procedure that can be applied for ASD drug formulations. We have demonstrated the effectiveness of this acoustic fusion process by generating amorphous solid dispersions of various BCS class 2 and 4 drug candidates, including torcetrapib, itraconazole, and lopinavir, with a variety of polymer systems, including HPMCAS (L, M, and H), copovidone, Soluplus®, PEG1500, Vitamin-E TPGS, Kolliphor EL, and Eudragit, etc. Formulations of these ASD drug products demonstrated significantly elevated solubility of the drug substance compared to the solubility of the crystalline form of the drug. Acoustic fusion products using the model drug torcetrapib in either HPMCAS-LF, copovidone + Vitamin-E TPGS, or Soluplus®, exhibited enhanced supersaturation solubility in aqueous buffer in vitro compared to the drug in crystalline form, indicating that the acoustic fusion process resulted in an amorphous solid dispersion state similar to those formed in spray drying (SD) or hot melt extrusion (HME) processes.
Homepage: https://www.selleckchem.com/
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