Objective: Carvedilol an antihypertensive drug, exhibits poor solubility and dissolution rate. Hence an attempt has been made to prepare the Cocrystals of Carvedilol to increase the solubility and dissolution rate. Methods:The Co-crystals of Carvedilol were prepared using coformer such as succinic acid, fumaric acid and oxalic acid by Solvent evaporation method. The prepared Co-crystals were evaluated for solubility, dissolution rate and micrometric properties. The Co-crystals were characterized by scanning electronic Microscopy (SEM), FT-Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffractometry (XRD).Results: SEM of pure carvedilol and Cocrystals morphology clearly showed the formation of a new solid phase with the coformer. The FT-IR spectra indicate the shifting of characteristic peak in the Co-crystals but does not show any interaction between the co-former used. DSC data showed the change in the endotherm with the melting point of Co-crystals. XRD spectra indicate the notified difference in the 2θ and the intensity of the peaks. Solubility of CAR-SA Cocrystals (2.225±0.35), CAR-FA Cocrystals (1.880±0.20) and CAR-OA Cocrystals (1.128±0.23) was markedly improved compared to pure Carvedilol (0.376±0.06). Thus the increased in dissolution rate for CAR-SA Cocrystals (93.72 %). was highest whereas CAR-FA Cocrystals (91.56 %), CAR-OA Cocrystals (88.93 %) compared to pure Carvedilol (40.3) within 60 Min. The Carvedilol cocrystals were also showed improvement in the flow properties compare to pure Carvedilol. Conclusion:Hence the Co-crystal formation could be helpful to improve the solubility, dissolution and micromeritic properties of Carvedilol.
Cancer immunotherapy has advanced significantly in recent years. Nanocarriers like liposomes are able to improve cancer immunotherapy and even stronger immune responses by improving cell type-specific distribution. Liposomes are lipid bilayer vesicles that are biodegradable and biocompatible and are often used as smart delivery systems for both hydrophobic and hydrophilic bioactives. Whereas the idea of employing liposomes for administering drugs has been known since the 1960s, the early 2000s saw continuing technological advances and formulations for drug entrapment and manufacturing. Modern deterministic studies have tried to discover more of how genetic material is delivered through liposomes. Liposomes' interactions with cells are still a bit of mystery. Liposome-mediated transmission of genetic material experiences systemic impediments in accordance with lysosomal degradation, endosomal escape, and nuclear uptake. Controlling the physical architecture and chemical properties of liposome structures, such as lipid-to-DNA charge, ester bond composition, size, and ligand complexation structure, is critical for targeting liposomes' success as vehicles for gene delivery. This analysis focuses on advancements in ligand-targeted liposomes and theranostic(diagnostic) liposomes for cancer diagnosis and treatment. We will explore the numerous transgenes mechanisms and molecular targets that are implicated in cancer cell death in this review, as well as the associated benefits with using liposomal formulations over through the years. This sequence of breakthroughs will be of interest to aspiring researchers and the pharmaceutical industry involved in liposome development.
Objectives: To avoid the first-pass metabolism of the drug (lurasidone HCl) and further improving its contact time with the nasal mucosa, intranasal mucoadhesive microspheres were developed by using natural (chitosan) and synthetic (Eudragit L 100) polymers by spray-drying method. The study aims to enhance the systemic drug absorption via the nasal membrane and to further evaluate the effect of polymers on the drug release profile. Methodology: The microspheres of each polymer were prepared in three different ratios with one blank batch, where the effect of concentration of polymer was assessed with all six formulations with respect to change in particle size and entrapment efficiency. The prepared microspheres were assessed for the essential parameters such as particle size, production yield, entrapment efficiency and histopathological study. The excipients-drug substance compatibility was assessed and their associative behavior was comprehensively studied by Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscopy (SEM). Results: The particle size analysis also revealed that all the formulations had particle size in the range of 10-15 μm which is suitable for intranasal administration. The optimized batch of chitosan microspheres (CH-2) and optimized batch of Eudragit L 100 microspheres (EU-1) formulations showed maximum drug loading of 68.3% and 74.9% whereas the cumulative drug release was found to be 76.36% and 80.18%, respectively. Conclusion: From the obtained results, it was concluded that the study showed a satisfactory attempt to formulate mucoadhesive microspheres with improved absorption rate and contact time of drug with nasal mucosa.
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