A solid dispersion based on milk-micelle as a drug-carrier for the enhancement of the aqueous solubility of ritonavir

The goal of present investigation was to evaluate the feasibility of formulating a solid-dispersion using milk-micelles as drug-carriers, to enhance the aqueous solubility of ritonavir

Formulation of a drug-phospholipid complex (Naturosome) to enhance the aqueous solubility of standardized extract of Centella asiastica (SCE)

Purpose: To evaluate the enhancement of aqueous solubility of standardized extract of Centella asiastica, a natural drug with known anti- Alzheimer’s activity, by formulating its complex (Naturosome) with a phospholipid - Phospholipon® 90H

The enhancement of the aqueous solubility of ritonavir via formulation of a drug-phospholipid complex

Objective: To evaluate the enhancement of aqueous solubility of a poorly water soluble drug ritonavir by forming its complex with a phospholipid (Phospholipon®90H)

The role of phospholipid as a solubility- and permeability-enhancing excipient for the improved delivery of the bioactive phytoconstituents of Bacopa monnieri

In an attempt to improve the solubility and permeability of Standardized Bacopa Extract (SBE), a complexation approach based on phospholipid was employed. A solvent evaporation method was used to prepare the SBE-phospholipid complex (Bacopa Naturosome, BN). The formulation and process variables were optimized using a central-composite design. The formation of BN was confirmed by photomicroscopy, Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD). The saturation solubility, the in-vitro dissolution, and the ex-vivo permeability studies were used for the functional evaluation of the prepared complex. BN exhibited a significantly higher aqueous solubility compared to the pure SBE (20-fold), or the physical mixture of SBE and the phospholipid (13-fold). Similarly, the in-vitro dissolution revealed a significantly higher efficiency of the prepared complex (BN) in releasing the SBE (\u3e 97%) in comparison to the pure SCE (~ 42%), or the physical mixture (~ 47%). The ex-vivo permeation studies showed that the prepared BN significantly improved the permeation of SBE (\u3e 90%), compared to the pure SBE (~ 21%), or the physical mixture (~ 24%). Drug-phospholipid complexation may thus be a promising strategy for solubility enhancement of bioactive phytoconstituents

Glucosamine HCl-based solid dispersions to enhance the biopharmaceutical properties of acyclovir

The objective of the work presented here was to assess the feasibility of using glucosamine HCl as a solid-dispersion (SD) carrier to enhance the biopharmaceutical properties of a BCS class III/IV drug, acyclovir (ACV). The solid-dispersions of acyclovir and glucosamine HCl were prepared by an ethanol-based solvent evaporation method. The prepared formulations characterized by photomicroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transforms infrared spectrophotometry (FTIR), powder x-ray diffractometry (PXRD) and drug content analysis. The functional characterization of ACV-SD was performed by aqueous solubility evaluation, dissolution studies, fasted versus fed state dissolution comparison, ex vivo permeability, and stability studies. Photomicroscopy and SEM analysis showed different surface morphologies for pure ACV, glucosamine HCl and ACV-SD. The physical-chemical characterization studies supported the formation of ACV-SD. A 12-fold enhancement in the aqueous solubility of ACV was observed in the prepared solid dispersions, compared to pure ACV. Results from in vitro dissolution demonstrated a significant increase in the rate and extent of ACV dissolution from the prepared ACV-SD formulations, compared to pure ACV. The rate and extent of ACV permeability across everted rat intestinal membrane were also found to be significantly increased in the ACV-SD formulations. Under fed conditions, the rate and extent of the in vitro dissolution of ACV from the formulation was appreciably greater compared to fasted conditions. Overall, the results from the study suggest the feasibility of utilizing glucosamine HCl as a solid dispersion carrier/excipient for enhancement of biopharmaceutical properties of acyclovir, and similar drugs with low solubility/permeability characteristics

Evaluation of Antidiabetic Potential of Ipomoea turpethum R.Br. and Ipomoea batata L. (Convolvulaceae) in Alloxan Induced Diabetes in Rats: A Comparative Study

ABSTRACT In order to explore the intra-genera variation for biological activity, the antidiabetic activity of Ipomoea turpethum and Ipomoea batata was carried out in alloxan induced diabetes in rats. Dried powdered material of both plants was defatted with petroleum ether 60-80 °C and cold macerated with hydro-ethanol for seven days. These extracts were screened for antidiabetic activity using alloxan induced diabetes in rats. Diabetes was induced by intra-peritoneal administration of alloxan monohydrate (120 mg/kg) on days 1 and 12 and blood glucose levels were estimated on 15 th day. Hydro-ethanol extracts of both the plants at the dose of 500 mg/kg, oral, significantly lowered the blood glucose levels in diabetic rats treated for 7 days. The antidiabetic activity of these plants was insignificantly different from each other. This suggests that, different species from same genera may have similar chemical constituents and pharmacological activity

Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

The aim of the present study was to develop and evaluate a thermoresponsive depot system comprising of docetaxel-loaded cubosomes. The cubosomes were dispersed within a thermoreversible gelling system for controlled drug delivery. The cubosome dispersion was prepared by dilution method, followed by homogenization using glyceryl monooleate, ethanol and Pluronic® F127 in distilled water. The cubosome dispersion was then incorporated into a gelling system prepared with Pluronic®F127 and Pluronic® F68 in various ratios to formulate a thermoresponsive depot system. The thermoresponsive depot formulations undergo a thermoreversible gelation process i.e., they exists as free flowing liquids at room temperature, and transforms into gels at higher temperatures e.g., body temperature, to form a stable depot in aqueous environment. The mean particle size of the cubosomes in the dispersion prepared with Pluronic® F127, with and without the drug was found to be 170 and 280 nm, respectively. The prepared thermoresponsive depot system was evaluated by assessing various parameters like time for gelation, injectability, gel erosion, and in-vitro drug release. The drug-release studies of the cubosome dispersion before incorporation into the gelling system revealed that a majority (∼97%) of the drug was released within 12 h. This formulation also showed a short lag time (∼3 min). However, when incorpo- rated into a thermoresponsive depot system, the formulation exhibited an initial burst release of∼21%, and released only∼ 39% drug over a period of 12 h, thus indicating its potential as a controlled drug delivery system

Commercially and medicinally significant aquatic macrophytes: Potential for improving livelihood security of indigenous communities in northern Bihar, India

The dispersed wetlands in the Darbhanga District of northern Bihar, India, provide a diversity of niches supporting substantial floral and faunal richness. The aquatic macrophytes of a representative range of perennial water bodies were surveyed fortnightly from June to September 2019, supported by a market survey undertaken with local stakeholders. A total of 61 species of vascular macrophytes was recorded, the majority of them Angiosperms (33 species of Dicotyledons from 21 families, and 26 Monocotyledons from 13 families) and two were Pteridophytes. This paper highlights the distribution pattern and potential commercial and medicinal values of aquatic macrophytes found in different wetland systems in northern Bihar. It further stresses their importance for subsistence, medicinal and economic purposes supporting the livelihoods of local people. Current trends and risks contributing to the degradation and loss of this diverse flora and its supporting habitats are considered. We recommend further assessment of the occurrence and values of this botanical resource, and extension of valuation to encompass the diverse additional ecosystem service benefits provided by the region’s wetland systems, as a basis for wetland conservation strategies founded on sustainable management and wise use, with particular reference to the potential for enhancing livelihood security of indigenous communities

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

In the present study, a phospholipid-based complex of standardized Centella extract (SCE) was developed with a goal of improving the bioavailability of its phytoconstituents. The SCE-phospholipid complex was prepared by solvent evaporation method and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy, and powder x-ray diffraction (PXRD) were used to confirm the formation of Centella naturosome (CN). The prepared complex was functionally evaluated by apparent solubility, in vitro drug release, ex vivo permeation, and in vivo efficacy studies. The prepared CN exhibited a significantly higher (12-fold) aqueous solubility (98.0 ± 1.4 μg/mL), compared to the pure SCE (8.12 ± 0.44 μg/mL), or the physical mixture of SCE and the phospholipid (13.6 ± 0.4 μg/mL). The in vitro dissolution studies revealed a significantly higher efficiency of CN in releasing the SCE (99.2 ± 4.7, % w/w) in comparison to the pure SCE (39.2 ± 2.3, % w/w), or the physical mixture (42.8 ± 2.09, % w/w). The ex vivo permeation studies with the everted intestine method showed that the prepared CN significantly improved the permeation of SCE (82.8 ± 3.7, % w/w), compared to the pure SCE (26.8 ± 2.4, % w/w), or the physical mixture (33.0 ± 2.7, % w/w). The in vivo efficacy studies using the Morris Water Maze test indicated a significant improvement of the spatial learning and memory in aged mice treated with CN. Thus, drug-phospholipid complexation appears to be a promising strategy to improve the aqueous solubility and bioavailability of bioactive phytoconstituents