Formulation and development of plasma volume expander using natural and modified starch from Solanum tuberosum.

BACKGROUND: To formulation and development of plasma volume expander (PVE) by using natural and modified starch from Solanum tuberosum. The function of blood circulation is to provide the needs of the body tissues and to maintain an appropriate environment in all tissue fluids of the body for the optimal survival and functions of the cells. Rapid restoration of the blood volume is necessary to decrease reduction in the amount of the blood. The PVEs are isotonic colloidal solutions, act by increasing the osmotic pressure of the intravascular compartment, which leads to the influx of the interstitial fluids through the capillary pore which, in turn, leads to the increase in the volume of the blood. Therefore, there is a need to discover the PVE with less side effects. The main aim of the present study is to use amylopectin as PVEs, fractionated from natural and modified starch obtained from S. tuberosum. METHODS: The starch extracted from the normal grains and the tubers of potatoes was selected for the production of starch. Statistical analysis includes in vitro characterization that involves viscosity studies, plasma-product interaction, osmotic pressure detection, molecular weight-viscosity relationship, determination of weight average molecular weight, enzymatic interaction, and in vivo characterization such as toxicity studies and the effect of the products on the blood coagulation. The isolated starch and fractionated amylopectin were analyzed for the physicochemical characteristics. RESULT AND CONCLUSION: The amylopectin fractionated from isolated starch from grains and tubers of potatoes can be used as PVE, as per the outcome of the study.

Floating-bioadhesive gastroretentive Caesalpinia pulcherrima-based beads of amoxicillin trihydrate for Helicobacter pylori eradication.

CONTEXT: An oral dosage form containing floating bioadhesive gastroretentive microspheres forms a stomach-specific drug delivery system for the treatment of Helicobacter pylori. OBJECTIVES: To prepare and evaluate controlled release floating bioadhesive gastroretentive chitosan-coated amoxicillin trihydrate-loaded Caesalpinia pulcherrima galactomannan (CPG)-alginate beads (CCA-CPG-A), for H. pylori eradication. MATERIALS AND METHODS: CCA-CPG-A beads were prepared by ionotropic gelation, using 2(3) factorial design with quantity of drug, combination of CPG with sodium alginate and concentration of calcium chloride as variables. Beads facilitated mucoadhesion to gastric mucosa with floating nature caused by chitosan coating for wide distribution throughout GIT. Developed beads were evaluated for characteristics like beads size-morphology, entrapment efficiency, DSC, XRD, FTIR, swelling ratio, in vitro mucoadhesion, in vitro drug release, in vitro floating and in vitro H. pylori growth inhibition studies. CCA-CPG-A beads were studied in Wistar rats for in vivo gastric mucoadhesion, in vivo H. pylori growth inhibition studies using PCR amplification of isolated DNA, rapid urease test. RESULT: Developed beads possess drug release of 79-92%, entrapment efficiency of 65-89%, mucoadhesion of 61-89%. In vivo mucoadhesion study showed more than 85% mucoadhesion of beads even after 7th hour. In vitro-in vivo growth inhibition study showed complete eradication of H. pylori. DISCUSSION: CPG-alginate and chitosan in beads interacts with gastric mucosubstrate surface for prolonged gastric residence with floating bioadhesion mechanism for H. pylori eradication in rats. CONCLUSION: Floating bioadhesive CCA-CPG-A beads offer a promising drug delivery system for H. pylori eradication at lower dose, reduced adverse effect and enhance bioavailability.

Bioavailability enhancement of ondansetron after nasal administration of Caesalpinia pulcherrima-based microspheres.

CONTEXT: Natural polymers have attracted a great deal of attention for use as potential carriers in site-specific delivery over past decades. Mucoadhesive microspheres are useful tools for nasal drug delivery. OBJECTIVES: To prepare and evaluate mucoadhesive microspheres as mode for nasal delivery of ondansetron using Caesalpinia pulcherrima galactomannan (CPG). MATERIALS AND METHODS: Conventional spray-dried CPG nasal microspheres loaded with ondansetron for intranasal drug delivery in order to avoid the first pass metabolism with improved therapeutic efficiency in treatment of nausea and vomiting as an alternative therapy to parenterals. Developed microspheres were evaluated for characteristics like particle size, entrapment efficiency, zeta potential, swelling ability, in-vitro mucoadhesion, in-vitro drug release, DSC, XRD study and histopathological evaluation of tissue. CPG-based ondansetron microspheres were studied in rabbits for screening nasal absorption potential of nasal formulation. RESULTS: Developed nasal microspheres possess entrapment efficiency of 80-89%, higher mucoadhesion of 72-84% across goat nasal mucosa. In-vivo study showed that microspheres based on mucoadhesive polymer were able to promote quick drug absorption as well as enhanced bioavailability of drug. DISCUSSION: Histopathological studies evaluated biocompatible and nontoxic nature of CPG in nasal cavity. Developed mucoadhesive microspheres by nasal route showed enhancement of bioavailability as compared to oral route in rabbits. CONCLUSION: CPG-based mucoadhesive microspheres can successfully deliver ondansetron intranasally, sustain its effect, avoid first pass effect, an alternative route of administration to injection and thus enhance systemic bioavailability of ondansetron hydrochloride.

Rheological characterization of galactomannans extracted from seeds of Caesalpinia pulcherrima.

The galactomannan from the seeds of Caesalpinia pulcherrima L. was isolated and purified by precipitation method using alcohol to get C. pulcherrima (CP) gum. CP gum was studied for its physicochemical and rheological properties. The composition of CP gum was found to contain mannose:galactose:glucose:xylose in a proportion of 2.8:1:0.1:0.08, with M/G ratio 2.80. The molecular weight (Mw) for CP gum was obtained to be approximately 2.72×10(6) Da by static light scattering measurements and 2.79×10(6) Da using Mark-Houwink relationship. The intrinsic viscosity by Huggins and Kraemer plots using capillary viscometry was obtained as 12-12.5 dl/g. The rheological behavior of aqueous galactomannan solutions was studied at 25°C, using steady-shear and dynamic oscillatory measurements. The various concentrations of CP gum exhibits shear thinning non newtonian behavior at high shear rate and newtonian flow at low shear rate. Experimental data in steady shear has been correlated and found a better fitting with the Cross and Carreau models. A graph of the specific viscosity at zero shear rate (η(sp0)) against coil overlap parameter (C[η]) was plotted and the slope of the lines in dilute and semi-dilute regions were found to be 1.23 and 4.1 respectively. The critical concentration (C*) was found to be about 3.8/[η]. The linear viscoelastic region for CP gum solutions presented nature as that of macromolecular solutions. At all shear rates and frequencies, η(ap) and η* had almost similar magnitudes, which shows its reasonable agreement with the Cox-Merz rule. The present investigation shows the suitability of CP gum as a pharmaceutical aid application like viscosity modifier, release retardants, binders.