Development of Lipid Polymer Hybrid Nanoparticles of Abietic Acid: Optimization, In-Vitro and Preclinical Evaluation.

The objective of the current research was to develop abietic acid (AA)-loaded hybrid polymeric nanoparticles (HNPs) for anti-inflammatory and antioxidant activity after oral administration. AAHNPs were developed by microinjection technique and optimized by 3-factor 3-level Box-Behnken design. The AAHNPs were evaluated for morphology, FTIR, X-ray diffraction, in-vitro release, ex-vivo permeation, in-vitro antioxidant, and in-vivo anti-inflammatory activity. The optimized AAHNPs (AAHNPsopt) displayed 384.5 ± 6.36nm of PS, 0.376 of PDI, 23.0 mV of ZP, and 80.01 ± 1.89% of EE. FTIR and X-ray diffraction study results revealed that AA was encapsulated into a HNPs matrix. The AAHNPsopt showed significant (P < 0.05) high and sustained release of AA (86.72 ± 4.92%) than pure AA (29.87 ± 3.11%) in 24h. AAHNPsopt showed an initial fast release of AA (20.12 ± 3.07% in 2h), which succeeded in reaching the therapeutic concentration. The AAHNPsopt showed 2.49-fold higher ex-vivo gut permeation flux than pure AA due to the presence of lipid and surfactant. The AAHNPsopt exhibited significantly (P < 0.05, P < 0.01, P < 0.001) higher antioxidant activity as compared to pure AA at each concentration. AAHNPsopt formulation displayed a significantly (P < 0.05) higher anti-inflammatory effect (21.51 ± 2.23% swelling) as compared to pure AA (46.51 ± 1.74% swelling). From the in-vitro and in-vivo finding, it was concluded that HNPs might be a suitable carrier for the improvement of the therapeutic efficacy of the drug.

Novel Products as Promising Therapeutic Agents for Angiogenesis Inhibition.

OBJECTIVE: Angiogenesis is the process of forming new blood vessels from pre-existing vessels and occurs during development, wound healing, and tumor growth. In this review, we aimed to present a comprehensive view of various factors contributing to angiogenesis during carcinogenesis. Anti-angiogenesis agents prevent or slow down cancer growth by interrupting the nutrients and blood supply to the tumor cells, and thus can prove beneficial for treatment. METHOD: The discovery of several novel angiogenic inhibitors has helped to reduce both morbidity and mortality from several life-threatening diseases, such as carcinomas. There is an urgent need for a new comprehensive treatment strategy combining novel anti-angiogenic agents for the control of cancer. The article contains details of various angiogenic inhibitors that have been adopted by scientists to formulate and optimize such systems in order to make them suitable for cancer. RESULTS: The results of several researches have been summarized in the article and all of the data support the claim that anti-angiogenic agent is beneficial for cancer treatment. CONCLUSION: This review focuses on novel antiangiogenic agents that play a crucial role in controlling carcinogenesis.

Syrupy herbal formulation of green bean pod extract of Phaseolus vulgaris L.: Formulation optimization by central composite design, and evaluation for anti-urolithiatic activity.

The green bean pods of Phaseolus vulgaris L. are traditionally used as a folk remedy for treating calcium oxalate kidney stones. The current research aimed to develop a syrup formulation containing green bean pod extract for anti-urolithiatic activity. The syrup was prepared using a simple blending method and optimized through a central composite design (CCD) with two independent variables: the ratio of pod juice (PJ) to sugar solution (SS) ranging from 1:0.5 to 1:1.5, and the percentage of CMC from 0.2% to 0.4% w/v. These variables were analyzed for their impact on viscosity (CP) and sedimentation percentage, helping to identify the best formulation out of 13 variants. The finalized formulation (F-opt) underwent assessment for physicochemical characteristics such as organoleptic properties, viscosity, density, sedimentation rate, and stability. Additionally, a microbiological assessment was performed utilizing the spread plate method. Further, it was evaluated for in vitro, ex vivo, and in vivo anti-urolithiatic activity in rat models for 28 days and compared with that of the reference standard (Cystone syrup). Additionally, acute toxicity was assessed in albino Swiss mice. Histopathological evaluations were then conducted on the kidneys of the Wistar rats that had been used for the in vivo studies, providing insight into the treatment effects on kidney tissue structure. The optimized formulation (F-opt) was a green, viscous, clear syrup with a pH of 5.8, a viscosity of 256.38 CP, a density of 1.31 g/ml, and a sedimentation rate of 0.69%. The optimized formulation was found to be stable, showing no significant changes in physicochemical and microbiological properties. The results of the in vitro, ex vivo, and in vivo anti-urolithiatic studies indicated that the optimized formulation effectively inhibited the aggregation of calcium oxalate. The acute toxicity studies revealed no mortality or adverse effects for both the optimized formulation and pure bean pod juice at a dose of 2000 mg/kg body weight. Histopathological examination revealed that rats treated with the optimized formulation exhibited a significant reduction in both the number and size of calcium oxalate deposits within various parts of the renal tubules. It can be concluded that the syrupy formulation of Phaseolus vulgaris L. green bean pod extract demonstrated significant anti-urolithiatic activity. This activity could be due to its diuretic properties and its ability to inhibit the formation of calcium oxalate crystals. However, limitations of the study included a lack of elucidation of the mechanism and limited generalizability of the findings.

Glyceryl behenate-based solid lipid nanoparticles as a carrier of haloperidol for nose to brain delivery: formulation development, in-vitro, and in-vivo evaluation

Abstract This study was aimed to develop the haloperidol (HPL) loaded solid lipid nanoparticles (SLNs) for brain targeting through the intranasal route. SLNs were fabricated by the emulsification diffusion technique using glyceryl behenate as lipid and tween 80 as a surfactant. SLNs were evaluated for particle size, zeta potential, structure, entrapment efficiency, solid state characterization by differential scanning calorimetry (DSC), and in-vitro release. In-vivo biological evaluation was performed on albino Wistar rats for the determination of pharmacokinetic as well as brain targeting parameters. Particle size, PDI, zeta potential, and entrapment efficiency of optimized formulation (HPL-SLNs 6) were found to be 103±09 nm, 0.190±0.029, -23.5±1.07 mV, and 79.46±1.97% respectively. In-vitro drug release studies exhibited that 87.21± 3.63% of the entrapped drug was released from the SLNs within 24 h. DSC curves confirmed that during entrapment in SLNs, the drug was solubilized in the lipid matrix and converted into the amorphous form. Enhanced HPL targeting to the brain was observed from HPL-SLNs as compared to HPL-Sol when administered intranasally. The value of AUC 0-∞ in the brain for HPL-SLNs i.n. was found to be nearly 2.7 times higher than that of HPL-Sol i.v., whereas 3.66 times superior to HPL-Sol administered i.n. Stability studies revealed that the formulation remains unchanged when stored at 4±2 °C (refrigerator) and 25±2 °C /60 ±5% RH up to six months. Finally, it could be concluded that SLN is a suitable carrier for HPL with enhanced brain targeting through i.n administration, as compared to the HPL-Sol, administered i.n. and i.v.