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Starch is found almost in all organs of plants as a carbohydrate reserve. It is considered one of the most commonly used pharmaceutical additives, mainly in tablet dosage forms; it used as a tablet binder when incorporated through the wet granulation process or as a disintegrant. Cajanus cajan has a high level of carbohydrate, which makes it another potential choice as a source for starch. This study aims to investigate and optimize the effect of Cajanus cajan starch concentrations as well as wet massing granulation time on physicochemical properties of metronidazole tablets. The hardness, friability percentage, and disintegration time of prepared tablets were determined, and the central composite design was employed in the optimization process. Then the tablets of optimized batch were compared against those tablets in which maize starch and sodium starch glycolate were used instead of Cajanus cajan starch. The results indicated that metronidazole tablets containing the upper level of starch paste (Cajanus cajan and/or maize starch paste) exhibited better percentage friability, hardness, and disintegration time than those formulated with lower levels and those without starch paste. The study showed that experimental design is a useful technique for optimizing Cajanus cajan starch-based tablets, which enabled a better understanding of how different variables could affect the responses. In addition, the study demonstrated that incorporation of Cajanus cajan starch in tablets formulation led to improvement of its physical properties compared to the formulations of maize starch and sodium starch glycolate respectively.

Objectives The main objective of present review is to explore and evaluate the effectiveness of recently developed methods to improve the bioavailability of orally administered biopharmaceutical drugs. Methods A systematic search of sciencedirect, tandfonline and Google Scholar databases based on various sets of keywords was performed. All results were evaluated based on their abstracts, and irrelevant studies were neglected during further evaluation. Results At present, biopharmaceuticals are used as injectable therapies as they are not absorbed adequately from the different routes of drug administration, particularly the oral one. Their insufficient absorption is attributed to their high molecular weight, degradation by proteolytic enzymes, high hydrophilicity and rigidity of the absorptive tissues. From industrial aspect incorporation of enzyme inhibitors (EIs) and permeation enhancers (PEs) and mucoadhesive polymers into conventional dosage forms may be the easiest way of formulation of orally administered macromolecular drugs, but the effectiveness of protection and absorption enhancement here is the most questionable. Conjugation may be problematic from regulatory aspect. Encapsulation into lipid-based vesicles sufficiently protects the incorporated macromolecule and improves intestinal uptake but have considerable stability issues. In contrast, polymeric nanocarriers may provide good stability but provides lower internalization efficacy in comparison with the lipid-based carriers. Conclusion It can be concluded that the combination of the advantages of mucoadhesive polymeric and lid-based carriers in hybrid lipid/polymer nanoparticles may result in improved absorption and might represent a potential means for the oral administration of therapeutic proteins in the near future.

Great interest been have develop to discover new excipients to solve problem that faced us during formulation like incompatibility and compressibility that lead to slow down manufacturing processes. Linseed mucilage has properties that suggested it as useful additives and binding agent like inertness, nontoxic and viscosity. The purpose of the present study was to extract and evaluate linseed mucilage as binding agent in prednisolone tablets. The Linseed mucilage was extracted and evaluated for physicochemical properties using official procedures. Tablet was prepared by wet granulation. Granules evaluation revealed satisfactory results. Three formula were prepared that contain three different percent from linseed mucilage 3%, 5% and 7%.The hardness test result show great increase in tablet hardness 4.23, 5.59 and 7.76, respectively. The dissolution test was carried in Ph 1.2 for 2 hours and cumulative drug release 20.33%, 17.88% and 14.49% respectively .And at Ph 6.8 for 4 hours cumulative drug release 78.18%, 75.43% and 69.19%. The tablets formulated showed acceptable general appearance. Formula mucilage 7% showed the best flowbility of granules, hardness and friability when compared with formulas 3% and 5%.In weight variation test indicated that the type and concentration of mucilage used were not significant. When increase the percent of mucilage in formula combined with increase in tablet hardness. Invitro dissolution study indicated that the main factors which influence the amount of drug released were the pH of the medium used and concentration of the mucilage.

The objective of this work was to extract and to investigate the physicochemical properties of Cajanus cajan starch (CCS) for use as pharmaceutical excipient and to compare its properties with official maize starch. Cajanus cajan seeds yielded 32.6 % starch on dry weight basis and several physicochemical characteristics of the extracted CCS and maize starch were evaluated such as: pH, moisture content, cold water solubility, swelling capacity, hydration capacity, moisture uptake, Amylose/Amylopectin ratio, flow properties and bulk and tapped densities. Also, the microphotograph and Fourier transform infrared (FTIR) had been taken for both starch samples. The physicochemical properties of CCS compared favorably with those of maize starch, suggesting that CCS can be used as tablet excipient in pharmaceutical industries.

The aim of this study was to characterize carboxymethyl cajanus cajan starch (CMCCS) and evaluate its capacity as binder, using metronidazole as model drug. Wet granulation method was adopted in preparation of metronidazole tablets containing CMCCS. Native cajanus cajan starch (NCCS) was carboxymethylated using monochloroacetic acid (MCA) and sodium hydroxide. Also the effect of CMCCS concentration and wet massing time on the physical properties of metronidazole (200 mg) tablet formulations was tested in a 22 full factorial design. The degree of substitution, amylose content, moisture content, pH and moisture uptake of CMCCS were found to be 0.252, 20.92%, 8.86 %, 6.9 and 48.5 respectively. Also CMCCS dissolved in cold water forming viscous solution. Similarly amylose content, moisture content, pH and moisture uptake of NCCS were 32.9%, 9.6 %, 6.12 and 17.34% respectively. in terms of bulk density, NCCS gave higher values compared to CMCCS. The values of Hausner ratio were 1.42 and 1.46 for NCCS and CMCCS respectively. The results of angle of repose revealed that the CMCCS had good flow characteristics, while the NCCS had passable flow characteristics. FT-IR analysis of the CMCCS sample showed peak shifting compared to the NCCS sample indicating carboxymethylation. CMCCS with degree of substitution (DS) of 0.252 was synthesized and it was further evaluated as tablet excipient in metronidazole based tablets. The results of quality control tests which performed for metronidazole formulations that prepared by CMCCS as binder, showed that the increase of CMCCS concentration from 12.5 % to 17.5 % led to increase in hardness and decrease in % friability values significantly, but no significant effect on DT was observed when wet massing time was kept at 6 min but when wet massing time was increased to 12 min, DT was significantly increased. Also the increase of wet massing time from 6 to 12 min led to slight increase in tablets hardness. The % friability was decreased due to increasing in wet massing time only in formulations containing CMCCS at 17.5%. Also all the batches showed more 90 % drug release within 15 min. Generally, the physicochemical and functional properties of CMCCS and NCCS showing that both NCCS and CMCCS can be used as tablet excipient in pharmaceutical industries. With CMCCS having superior properties compared to unmodified cajanus cajan starch.

The oral delivery of biopharmaceuticals requires the including of absorption enhancer, protease inhibitor and a suitable carrier system. The aim of the present work was to formulate and characterize chitosan solutions/films incorporating citric acid (CA) as potential excipient in comparison to the well-known acetic acid (AA)-based films as a reference. Films were made by the solvent casting method with/without glycerol (G), propylene glycol (PG) and polyethylene glycol (PEG-400) as plasticizers. The minimum film forming temperature (MFFT) of the prepared solutions, film thickness, hardness/deformation, mucoadhesivity, moisture content, FT-IR spectra and surface free energy (SFE) were investigated. Chitosan has been reported as a safe and effective paracellular absorption enhancer for hydrophilic macromolecules, therefore there would be more rationale for incorporating CA as a solubility enhancer, a permeation enhancer and an enzyme inhibitor. CA shows good cross-linking, an ideal plasticizing property and increases both tensile strength and mucoadhesivity, thus its incorporation simplifies the formulation while improving effectiveness. We concluded that CA (3.5, 4 and 5 w/v %)-based chitosan solution could be used as a novel coating/subcoating polymer for oral macromolecule delivery, or as oral mucoadhesive films.

The aim of this study was to develop a delayed-release matrix pellet containing atenolol as active pharmaceutical ingredient. The matrix additionally contained trisodium phosphate dodecahydrate as alkalizing pore-former agent to enhance the dissolution of the atenolol at pH 6.8. The delayed release was ensured by coating with a gastro-resistant polymer. For this purpose, an acryl EZE MP aqueous dispersion was used, which is suggested in the literature for pellet coating. Before this functional film coating, a protective polymer layer was developed, to prevent direct contact between the alkalizing layer and the acryl EZE. The results of in vitro dissolution tests demonstrated that the double-coated pellet preparation is a delayed-release solid dosage form.

The aim of this study was to investigate the influence of the wetting liquid on the properties of pellets prepared by extrusion and spheronization. Different grades of ethylcellulose were used as matrix former, with microcrystalline cellulose as filler and atenolol as model active agent. Each ethylcellulose type was applied with water alone, or with a combination of water and ethanol. The formation of the matrix and the interaction of the components were evaluated via mechanical, dissolution and morphological studies on the pellets. The presence of ethanol in the wetting liquid led to a decrease in the liberation of the active agent in the first phase of the dissolution process, but also caused a reduction in the breaking hardness of the pellets. High viscosity grade ethylcellulose gave rise to a more relevant decrease in breaking hardness. The plasticity of the mass was influenced by variation of the wetting liquid.

The aim of this study was to investigate the effects of alkalizing components and the nature of the wetting liquid on the properties of matrix pellets prepared by extrusion and spheronization. Atenolol was used as an active pharmaceutical ingredient, ethylcellulose as a matrix former, microcrystalline cellulose as a filler and disodium phosphate anhydrous and trisodium phosphate dodecahydrate as alkalizing materials. Water and a water-ethanol mixture served as granulation liquids. Pellet formation was evaluated via mechanical, dissolution and morphological studies. In order to enhance the dissolution of Atenolol from the pellets, alkalizing components were used and the influence of these components on the pH was tested. Investigations of the breaking hardness, the morphology and the dissolution revealed that the pellets containing trisodium phosphate dodecahydrate and prepared with a higher amount of water as binding liquid displayed the best physico-chemical parameters and uniform dissolution. In in vitro experiments, the dissolution release complied with the texture of the pellets and the effect of pH. The pellets have suitable shape and very good hardness for the coating process and are appropriate for subsequent in vivo experiments.

The aim of this study was to investigate the effects of the parameters of the spheronization and the nature of the wetting liquid on the properties of matrix pellets prepared by extrusion and spheronization. Ethylcellulose was used as a matrix former, microcrystalline cellulose as a filler, atenolol as a model active agent, and water and a water–ethanol mixture as liquids. The formation of the pellets and the interactions of the components were evaluated via mechanical, dissolution and morphological studies on the pellets. A factorial design was used to determine the effects of the evaluated factors. It was concluded that significant effects were exerted not only by the operational parameters, but also by the nature of the liquid. The breaking hardness and the dissolution revealed that the ethanol in the liquid caused changes in the wettability of the components and consequently in the matrix structure. This was explained by a comparison of the relative importance of the factors. The alterations induced by ethanol were preferable in the dissolution, because the possibility of the burst effect in the first phase of dissolution can then be avoided. However, it is not favourable as concerns the sphericity and the mechanical properties of the pellets.

Medicinal plants have curative properties due to the presence of various complex chemical substance of different composition, which are found as secondary plant metabolites in one or more parts of these plants. Mangifera indica Linn (MI L.) is a species of mango in the Anacardiaceae family. Phytoconstituents in the seed extracts may be responsible for the antimicrobial activity of the plant. The purpose of the study was to formulate and evaluate the antimicrobial herbal ointment and cream from extracts of the seeds of mango (MI L.) The formulated ointments containing oleaginous-based showed the best formulation compared to the emulsion water in oil type, the ointment and cream bases in different concentration 1%, 5% and 10%. The formulated ointment and cream of MI L. were subjected to evaluation of Uniformity of Weight, measurement of pH, viscosity, Spreadability, Acute skin irritation study, stability study and antimicrobial activity. Our study shows that MI has high potential as an antimicrobial agent when formulated as ointment and creams for topical use. Thus, the present study concludes that the formulated formulations of the MI are safe and efficient carriers, with potent antimicrobial activity.