Assam Bora Rice Research Articles

Citric acid esterified Glutinous Assam bora rice starch enhances disintegration and dissolution efficiency of model drug

The current work was designed to study the starch's physicochemical attributes, tablet disintegration and dissolution efficiency and its derivatives obtained from the glutinous Assam bora rice (G-ABR) variety of Assam, Northeast India. Starch was isolated by a simple protein denaturation method, and a starch derivative was prepared through citric acid modification. G-ABRS and citrated G-ABRS were characterized through FTIR, DSC, XRD and SEM. The rate of consolidation, consolidation index, angle of internal friction, packing rearrangement and cohesive properties were determined to investigate their applications as functional excipients in pharmaceutical industries. G-ABRS and citrated G-ABRS exhibited better packing rearrangement and cohesive properties than standard corn starch. Furthermore, immediate release of API from the tablet compact was observed when the starch concentration increased from 1 to 5 %, indicating facilitation of the tablet compact disintegration. Therefore, G-ABRS and citrated G-ABRS are potentially functional and sustainable materials for pharmaceutical industries.

Tailoring of Colon Targeting with Sodium Alginate‐Assam Bora Rice Starch Based Multi Particulate System Containing Naproxen

AbstractThis research is focused on the formulation and optimization of Assam Bora rice starch (ABRS)‐alginate beads containing a non‐steroidal anti‐inflammatory drug (NSAID) such as Naproxen (NA), by an ionotropic gelation technique using 32 factorial design for colon targeting against rheumatoid arthritis, inflammatory bowel disease, and colon cancer. The impact of a polymeric blend of sodium alginate (SA) and ABRS on the drug entrapment efficiency (DEE, %), bead size (BS), and percentage cumulative drug release in the first 6 h (Q6, %) is optimized. The DEE (%) of all the developed beads is found to be in between 45.25% and 85.14% with an in vitro drug release of 32.81–42.18% in first 6 h. The optimized batches of beads are coated with Eudragit S100 (ES100) (5%, 10%, and 15% w/v) to facilitate colon targeting in a prominent way. The average size of the developed beads is found to be within the range of 751.61–822.22 µm. The optimized ABRS‐alginate beads containing NA show significant drug permeability over a prolonged period on ex vivo permeability through a goat colon. The in vivo roentgenographic study on rats shows the colon targeting of the beads without degradation.

Doxorubicin loaded carboxymethyl Assam bora rice starch coated superparamagnetic iron oxide nanoparticles as potential antitumor cargo

In recent years, polysaccharide-decorated superparamagnetic iron oxide nanoparticles (SPIONs) have gained attention in the field of “nanotheranostics” with integrated diagnostic and therapeutic functions. Carboxymethyl Assam bora rice starch-stabilized SPIONs (CM-ABRS SPIONs), synthesized by co-precipitation method, has already shown exciting potential towards magnetic drug targeting potential. After establishing it as a promisable targeting carrier, the present study is focused on the next step i.e. to evaluate its In vitro anti-tumor potential by loading anticancer drug “Doxorubicin hydrochloride (DOX)” onto CM-ABRS SPIONs. DOX-loaded CM-ABRS SPIONs were physico-chemically characterized by DLS, zeta-potential, TEM, FT-IR, XRD, and VSM analysis. Spectroflourimetric analysis confirmed the maximum loading of DOX up to 6% (w/w) onto CM-ABRS SPIONs via electrostatic interactions. Further, molecular level drug performance was investigated by docking study against receptors (HER-2 and Folate receptor-α) over expressed in cancer cells and MTT assay (in MCF-7 and HeLa cell line), which conferred promisable results of DOX-CM-ABRS SPIONs as compared to standard DOX solution.

Carboxymethyl Assam Bora rice starch coated SPIONs: Synthesis, characterization and in vitro localization in a micro capillary for simulating a targeted drug delivery system

Carboxymethyl Assam Bora rice starch coated superparamagnetic iron oxide nanoparticles (CM-ABRS SPIONs) were chemically synthesized by co-precipitation method and particle size reduction was controlled by high energy homogenization process. Effects of various process variables (polymer concentration, homogenization speed and cycles) were optimized on the basis of average particle size (Z-average) and polydispersity index (PDI) of CM-ABRS SPIONs. The optimized CM-ABRS SPIONs were characterized for their particle size, surface morphology, electrokinetic potential, chemical interactions, crystallinity, magnetic properties, and targeting potential in presence of external magnetic field. In vitro localization of CM-ABRS SPIONs in a suspension of FITC (Fluorescein isothiocyanate) labeled RBCs (Red blood cells; hematocrit value; 45% (v/v)) was conducted inside a square glass capillary (500 × 500 μm2 cross section) in the presence of an externally applied magnetic field (Ms = 150 mT), simulating the case of magnetic drug targeting (MDT) approach. The aggregation dynamics of CM-ABRS SPIONs inside a micro capillary was observed with respect to time (t = 0 to 600 s), which shows proportionality to time of exposure to the externally applied magnetic field. This in vitro study acts as an important platform for design and optimization of active targeted drug delivery system.

CHEMICAL MODIFICATION, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE POTENTIALITY OF ASSAM BORA RICE STARCH

Objective: The objective of the present study was to chemical modification, characterization and evaluation of mucoadhesive potentiality of Assam bora rice starch as potential excipients in the sustained release drug delivery system. Methods: The starch was isolated from Assam bora rice and esterified using thioglycolic acid and characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and Nuclear magnetic resonance (NMR). The 10% w/v gel formulation based on modified bora rice starch loaded with irinotecan (0.6%) was prepared and evaluated for various rheological properties, ex-vivo mucoadhesion using goat intestine and in vitro drug release study in phosphate buffer pH 6.8.Results: The chemical modification was confirmed by FT-IR and NMR studies with the presence of the peak at 2626.74 cm-1 and a singlet at 2.51 respectively due to–SH group. Ex-vivo mucoadhesion studies showed 6.6 fold increases in mucoadhesion of the modified starch with compared to native starch (46.3±6.79g for native starch; 308.7±95.31g for modified starch). In vitro study showed 89.12±0.84 % of drug release after 6 h in phosphate buffer pH 6.8 and the release kinetics followed Non-Fickian diffusion.Conclusion: The modified Assam bora rice starch enhanced a mucoadhesive property of the native starch and thus, can be explored in future as a potential excipient for the sustained release mucoadhesive drug delivery system.

Synthesis and characterization of novel carboxymethyl Assam Bora rice starch for the controlled release of cationic anticancer drug based on electrostatic interactions

Carboxymethyl Assam Bora rice starch (CM-ABRS) was chemically synthesized in non-aqueous medium with the optimum degree of substitution (DS) of 1.23, and physicochemically characterized by FT-IR, DSC, XRD, and SEM analysis. Comparative evaluation of CM-ABRS with native starch (ABRS) for powder flow characteristics, swelling index, apparent solubility, rheological properties, textural properties, and mucoadhesive studies were carried out. The aim of the current work was to investigate the potential of CM-ABRS as a novel carrier for the water-soluble chemotherapeutic, doxorubicin hydrochloride (DOX). Formation of drug/polymer complex (DOX-CM-ABRS) via electrostatic interaction has been evaluated for the controlled release of DOX in three different pH media (phosphate-buffered saline (PBS), pH 7.4, 6.8, and 5.5). In vitro drug release studies illustrated faster release of drug in PBS at pH 5.5 as compared to pH 6.8 and pH 7.4, respectively, indicating the importance of pH-sensitive drug release from the DOX-CM-ABRS complex in malignant tissues.

Assam Bora Rice Starch Based Biocompatible Mucoadhesive Microsphere for Targeted Delivery of 5-Fluorouracil in Colorectal Cancer

The aim of this study was to develop novel colon targeted mucoadhesive microspheres (MAMs) for site specific delivery of 5-fluorouracil (5-FU) to colon without the drug being released in the stomach or small intestine. MAMs were prepared using Assam Bora rice starch, a natural mucoadhesive polymer, by a double emulsion solvent evaporation method. The microspheres were characterized for their shape, size, surface morphology, size distribution, incorporation efficiency, and in vitro and in vivo drug release studies. The release study confirmed the insignificant release of 5-FU in physiological condition of stomach and small intestine and major drug release in the cecal content. In vivo release study of the optimized MAMs was compared with immediate release (IR) 5-FU. 5-FU was distributed predominantly in the upper GI tract from the IR, whereas 5-FU was distributed primarily to the lower part of the GI tract from the MAM formulation. Enhanced levels of liver enzymes were found in animals given IR 5-FU as well as augmented levels of serum albumin, creatinine, leucocytopenia and thrombocytopenia was also observed. Thus to sum up, it can be appropriately established that the 5-FU release pattern from MAMs exhibits slow and extended release over longer periods of time with reduced systemic side effects.

Colorectal cancer targeted Irinotecan-Assam Bora rice starch based microspheres: a mechanistic, pharmacokinetic and biochemical investigation

The purpose of this investigation was to evaluate the colon-targeted Irinotecan Hydrochloride (ITC-HCl) loaded microspheres by pharmacokinetic and biochemical studies. The microspheres were prepared by double emulsion solvent evaporation method with natural polymer Assam Bora rice starch. The microspheres were characterized for their micromeritics properties, incorporation efficiency, in vitro and in vivo drug release studies. The release study confirmed the insignificant release of ITC-HCl in physiological condition of stomach and small intestine and major drug release in the caecal content. In vivo release study of the optimized microsphere was compared with immediate release (IR) ITC-HCl. ITC-HCl was distributed predominantly in the upper GI tract from the IR, whereas ITC-HCl was distributed primarily to the lower part of GI tract from the microspheres formulation. Enhanced levels of liver enzymes were found in animals given IR ITC-HCl as well as augmented levels of serum albumin, creatinine, leucocytopenia and thrombocytopenia was also observed. In summary, Assam Bora rice starch microspheres exhibit slow and extended release of ITC-HCl over longer periods of time with reduced systemic side-effects.

Tableting Properties of Assam Bora Rice Starch

Starches are used as fillers, binders, and disintegrating agents in the tablet formulation due to their suitable physicochemical as well as mechanical properties. In the present investigation, a study has been done on the compaction properties of Assam Bora rice starch, and their physicochemical properties are evaluated. Assam Bora rice starch exhibit good flow properties. The influences of physical and geometrical properties of starch were evaluated with regard to their compression properties. Further compaction properties of the Assam Bora rice starch were evaluated by density measurement, Heckel and Kawakita equation. The result obtained shows that Assam Bora rice starch deforms mainly by plastic deformation. From the study it has been concluded that Assam Bora rice starch would be more useful in minimizing the problems of lamination and capping especially on high speed tableting machine with short dwelling time for the plastic deformation of material, on the other hand it would be more useful when high tensile strength of tablet is desirable.

Tableting Properties of Assam Bora Rice Starch

Starches are used as fillers, binders, and disintegrating agents in the tablet formulation due to their suitable physicochemical as well as mechanical properties. In the present investigation, a study has been done on the compaction properties of Assam Bora rice starch, and their physicochemical properties are evaluated. Assam Bora rice starch exhibit good flow properties. The influences of physical and geometrical properties of starch were evaluated with regard to their compression properties. Further compaction properties of the Assam Bora rice starch were evaluated by density measurement, Heckel and Kawakita equation. The result obtained shows that Assam Bora rice starch deforms mainly by plastic deformation. From the study it has been concluded that Assam Bora rice starch would be more useful in minimizing the problems of lamination and capping especially on high speed tableting machine with short dwelling time for the plastic deformation of material, on the other hand it would be more useful when high tensile strength of tablet is desirable. Keywords: Assam Bora rice starch, tableting properties, heckel plot, kawakita plot, compaction properties, plastic deformation, tapioca starch, corn starch

Compactibility and compressibility studies of Assam Bora rice starch

A comparison study was made on the powder flow characteristics, tableting properties of experimental Assam Bora rice starch, obtained from the variety Aghuni Bora of Oryza sativa and the mechanical properties of tablets made up of it with those of official Starch 1500®. The influences of physical and geometrical properties of both the starch were evaluated with regards to their compression properties. It has been found that Assam Bora rice starch reflects better physical characteristics such as higher bulk and tap densities, less porosity, better powder packing ability, minimum lubricant sensitivity, large surface area and improved flowability. Apart from that the mechanical properties, such as toughness and Young's modulus of Assam Bora rice starch were also compared with that of Starch 1500®. It has been also brought into result that compactibility of Assam Bora rice starch was not affected by the blending time. Further compaction properties of the experimental starch were evaluated by using Kawakita and Heckel equations and compared well with those of Starch 1500®. The result obtained shows that it mainly deforms by plastic deformation. Their onset of plastic deformation and strain rate sensitivity as compared to that of Starch 1500® demonstrates its potential use as a direct compression filler-binders.

In vitro and in vivo evaluation of Assam Bora rice starch-based bioadhesive microsphere as a drug carrier for colon targeting

Objective: The aim of this study is to develop, characterize and evaluate (in vitro and in vivo) a novel colon-targeted bioadhesive microsphere (BAM) containing metronidazole (MTZ).Methods: BAMs are prepared using Assam Bora rice starch as a natural bioadhesive polymer by a double emulsion solvent evaporation method.Results: The prepared microspheres showed a uniform spherical shape, with excellent retention time. The in vitro drug release study of the optimized formulations, in different physiological environments, confirmed the insignificant release of metronidazole in the physiological conditions of the stomach (10 – 12.5%) and small intestine (< 25%). Further, fast and major drug release in cecal content (> 90) indicated that the release of the drug was unaffected by the hostile environment of the gastrointestinal tract (GIT). In vitro bacterial inhibition studies illustrated that MTZ loaded BAMs, inhibiting metronidazole-sensitive Bacteroides fragilis and selected BAMs (F1 – F7), have an equivalent or higher zone of inhibition than the marketed formulation. An in vivo organ distribution study of MTZ revealed that Assam Bora rice starch-based microspheres were relatively intact in the upper part of GIT, and the drug was released only after reaching the colon, owing to the microbial degradation of Assam Bora rice starch by microflora residing in the colon.Conclusion: MTZ release patterns exhibited slow and extended release over longer periods of time, which shows the potential of Assam Bora rice starch microspheres as a drug carrier for an effective colon-targeted delivery system.

Feasibility of Assam Bora Rice Starch as a Compression Coat of 5-Fluorouracil Core Tablet for Colorectal Cancer

The colon and rectum are the parts of digestive system of human beings. Cancer affecting either of these organs may be called colorectal cancers. Conventional cancer chemotherapy is not very effective for treatment of colorectal cancer, as the drug molecule does not reach the target site at therapeutic concentration, on the other side they produces sever systemic toxic effect. Aim of this study was to develop a novel colon targeted Assam Bora rice starch compression coated tablet for site specific delivery of 5-FU to the colon without the drug being released in stomach or small intestine. Core tablet of 5-FU was prepared using microcrystalline cellulose (MCC) and spray dried lactose by direct compression method. The in vitro drug release study in different physiological environment confirmed insignificant release of 5-FU in physiological condition of stomach and small intestine further fast and major drug release in caecal content. In vivo drug absorption of optimized formulation was performed in order to establish its targeting potential in colon. It is concluded from the present study that Assam Bora rice starch can be used as a drug carrier for an effective colon targeted delivery system for drugs effective against the large intestine resident disease condition.

Development of Polysaccharide based Colon Targeted Drug Delivery System: Design and Evaluation of Assam Bora rice Starch based Matrix Tablet

The aim of this study was to develop a novel colon targeted matrix tablet containing Metronidazole (MTZ) as model drug. Matrix tablets were prepared using Assam Bora rice starch, which is essentially a natural polymer, by wet granulation technique. The granules prepared were subjected to evaluation for angle of repose, bulk density, compressibility index, Hausner's ratio, total porosity, and drug content. The developed tablets were also analysed for thickness, diameter, weight variation tests, tablet crushing strength, friability, and in vitro release studies. The granules displayed satisfactory flow properties, compressibility, Hausner's ratio and drug content. Almost all the tablet formulations showed acceptable pharmacotechnical properties and complied with the in-house developed specifications for the tested parameters. Drug release study confirmed to the initial fast release in the acidic environment of surface adhered drug followed by slow release in alkaline media subsequently leading to fast and major drug release in the caecal content. Furthermore, the release of drug was unaffected by the hostile environment of GIT which can be ascribed to microbial degradation, promptly followed by enzymatic degradation. Curve fitting proved that the drug release from the tablets followed the Higuchi model. In vitro bacterial inhibition studies illustrated that the released drugs were able to diffuse through agar medium, inhibiting MTZ sensitive Bacteroides fragilis. The selected MTZ matrix tablets (F1-F6) had zones of inhibition paralleling those of the marketed formulation.

Evaluation of Assam Bora Rice Starch as Plasma Volume Expander by Polymer Analysis

Water soluble polysaccharides are currently finding increasing use as a basis material for plasma volume expander. In clinical setting it is desirable to have a precise knowledge of steric and chemical structure, since these affect the pharmacokinetics and pharmacology of plasma volume expander. Branch component of starch amylopectin is very similar in structure to glycogen, the reserve polysaccharide of animal and therefore is liable to be compatible with body tissue. The knowledge of weight average molecular mass, degree of branching, osmotic pressure and coil dimension are essential, since low molecular mass do not have desirable effect and large molar mass have undesirable effect. Assam Bora rice starch was characterized by polymer analysis for use as plasma volume expander. Characterization involves the determination of FTIR spectra, degree of branching by H1 NMR, osmotic pressure by internal measurement technique, establishment of Mark-Houwink relationship and determination of Molecular weight - viscosity relationship.

Modeling and characterization of drug release from glutinous rice starch based hydrogel beads for controlled drug delivery

Purpose: To identify the potential of Assam Bora rice in modulation of drug release from the formulated matrix devices and demonstrate its utility in pharmaceutical drug carrier systems. Methods: The hydrogel microbeads were prepared by an industrially feasible conventional ionotropic gelation method using the blends of pregelatinized Bora rice along with sodium alginate as mucoadhesive backbone. The potential of proposed natural polymer in modulation of drug release from the formulated microbeads was investigated through in vitro dissolution test conducted as per SUPAC-MR guidelines provided by FDA. Data obtained from in vitro release studies were fitted to various kinetic equations to find out the kinetics and mechanism of drug release from fabricated microbeads. Results: The microbeads were almost spherical, discreet and free flowing in a size range of about 0.726±0.008 mm to 1.16±0.009 mm. The different formulations had variable correlation with the different kinetic models under the different release environments. Conclusion: Assam Bora can be a promising option for mucoadhesive controlled drug delivery systems as natural substance. Keywords: Drug delivery, Bora rice starch, Release kinetics, Natural polymer.

Isolation and Physicochemical Characterization of Assam Bora Rice Starch for Use as a Plasma Volume Expander

Water soluble polysaccharides are most effective oncotic agents which are used for treatment of intravascular volume deficiency. Nowadays, they are used as basic material for plasma volume expander. Plasma volume expander based on starch has lower tendency to remain in any major organ of body in comparison to other plasma volume expander. Branched component of starch amylopectin is very similar in structure to glycogen, the reserve polysaccharides of animal; for all this reason starch is compatible with body tissues. Physicochemical properties of raw starch and amylopectin, isolated from Assam Bora rice were characterized for use as plasma volume expander. Characterization involves the determination of ash value, weight average molecular mass, viscosity and resistance towards enzymatic (amylase) hydrolysis. Amylose content was almost negligible. The X-ray diffraction pattern of Assam Bora rice starch was typically A type. High degree of crystallinity of Assam Bora rice starch reflects its resistance towards enzymatic hydrolysis which is of therapeutic advantage for using it as a plasma volume expander.