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Purpose: The industrial applications of lipases are hampered by their sensitive nature to processing and storage conditions. In this context, this study presents a simple statistical modeling approach using Nano Spray Dryer BÜCHI B-90 as an ideal technique for the production of stable lipase nano-powder (LNP). Methods: In this study, factorial design is employed to optimize the spray drying process for Mucor racemosus lipase enzyme. Different variables were investigated such as adjuvant type (dextrin, mannitol, and lactose), concentration (2%, 4%, 8%), nozzle diameter, and inlet temperature (80 °C, 100 °C, 120 °C). Additionally, the physicochemical properties of LNP including particle size, residual enzyme activity, powder yield, morphology, and moisture content are investigated. Results: Results indicate a significant effect of additive type on product yield value and particle size. LNP exhibited a broad range of physical characteristics (enzyme residual activity 80.5–100%, particle size 210–1313 nm, and yield value 24–99%) and 98.4% residual activity after storage for 2 months at 5 °C. Scanning electron microscopy (SEM) images have shown a variation in the morphology of LNP with a remarkable flower-like structure in presence of lactose. The measured pronounced lipase stability is accredited to high local lipase concentration, adjuvant stabilizing effect, and favorable lipase conformation at the nano-scale-solid state. Conclusion: Based on the results presented, a robust approach for the production of a maximally viable spray-dried LNP in solid form can be employed for extended biotherapeutic and biotechnological applications of lipase. [ABSTRACT FROM AUTHOR]

The current study aimed to investigate the ability of chitosan/poly (acrylic acid) nanogel (CAN) to improve the bioavailability and anticancer potential of rutin. Synthesis of CAN was carried out by gamma radiation-induced polymerization of acrylic acid in an aqueous solution of chitosan. The relationship between the hydrodynamic radius of CAN and the absorbed radiation doses was also investigated. The prepared nanogels were characterized by transmission electron microscopy (TEM), dynamic light scattering (DLS), X-ray diffraction (XRD), and Fourier transform infrared (FT-IR) techniques, and then, it was used as a nano-drug carrier for rutin. The developed formulation was evaluated for its antitumor activity against chemically induced hepatocarcinoma in rats. The following parameters were measured: aspartate and alanine aminotransferase, alkaline phosphatase, gamma glutamyltransferase, and total bilirubin as liver function test; vascular endothelial growth factor as an angiogenesis marker; α-fetoprotein as a tumor marker; and P53, caspase-3, Bax, and Bcl-2 as apoptosis markers. Histopathological examination was also confirmed. Significant enhanced anti-proliferative, anti-angiogenic, and apoptotic effects were observed for rutin-loaded CAN than free rutin, indicating that this formulation could provide a novel therapeutic approach to serve as a promising agent for treatment of hepatocellular carcinoma. [ABSTRACT FROM AUTHOR]

In the present study, l-arginine/acrylic acid (Arg/AAc) batch hydrogel was successfully prepared by gamma irradiation for transdermal delivery of propranolol HCl in hypertensive rats. The resulted system has been characterized by FTIR to confirm the hydrogel formation. The swelling behavior of the prepared hydrogels was investigated as a function of time and pH. The kinetics of swelling has been investigated. In vivo pharmacokinetics evaluation, skin irritation test, and histopathological studies were investigated. Furthermore, the antihypertensive efficacy of transdermal propranolol-loaded Arg/AAc hydrogel on methyl prednisolone acetate-induced hypertensive rats was evaluated. It was found that the prepared patches exhibited a sustained release of the drug into systemic circulation over oral route which is subjected to hepatic first-pass metabolism, coupled with a short plasma half-life. Transdermal administration displayed a prolonged antihypertensive effect in spontaneously hypertensive rats. Moreover, the skin irritation test and histopathological examination indicated that the prepared patches are not irritant and can be safely applied on the skin. These results indicated that the hydrogel system composed of Arg and AAc has potential as a transdermal delivery system. [ABSTRACT FROM AUTHOR]

In an effort to increase the oral bioavailability of Amphotericin B (AmB), a pH-sensitive drug carrier composed of Tragacanth (Trag) and acrylic acid (AAc) was prepared using γ-irradiation. The swelling behavior of (Trag/AAc) hydrogels was characterized as a function of pH and ionic strength of the swelling medium. The obtained swelling indices revealed the ability of the prepared hydrogel to protect a loaded drug in stomach-simulated medium (Fickian behavior) and to release such drug in intestinal-simulated medium (non-Fickian behavior). In vitro release studies of the antifungal (AmB) were performed to evaluate the hydrogel potential as a drug carrier. The antifungal activity of the prepared oral formulation was investigated in a mouse model of systemic candidiasis. Data revealed that (Trag/AAc)-AmB has a potent antifungal efficacy as demonstrated by prolonging the survival time and reducing the tissue fungal burden, serum antibody titers, as well as inflammatory cytokines in kidney and liver tissues. Furthermore, in vivo toxicity of (Trag/AAc)-AmB was assessed via measuring kidney and liver functions, and results displayed the safety of this novel AmB formulation which was confirmed by histopathological examination. Overall, results indicated that the prepared (Trag/AAc)-AmB is an effective oral delivery system for AmB with better bioavailability and minimal toxicity and could represent a promising approach for improving the therapeutic index of the drug. [ABSTRACT FROM AUTHOR]