Anandrao R. Kulkarni

Biodegradable polymeric nanoparticles as drug delivery devices

This review presents the most outstanding contributions in the field of biodegradable polymeric nanoparticles used as drug delivery systems. Methods of preparation, drug loading and drug release are covered. The most important findings on surface modification methods as well as surface characterization are covered from 1990 through mid-2000.

Chemically modified polyacrylamide-g-guar gum-based crosslinked anionic microgels as pH-sensitive drug delivery systems : preparation and characterization

New spherically shaped cross-linked hydrogels of polyacrylamide-grafted guar gum were prepared by the emulsification method. These were selectively derivatized by saponification of the -CONH2 group to the -COOH group. The derived microgels were characterized by FTIR and elemental analyses. The derivatized microgels were responsive to pH and ionic strength of the external medium. The swelling of microgels increased when the pH of the medium changed from acidic to alkaline. Transport parameters, viz., solvent front velocity and diffusion coefficients were calculated from a measurement of the dimensional response of the microgels under variable pH conditions. The variation in pH changed the transport mechanism from Case II (in 0.1 N HCl) to non-Fickian (in pH 7.4 buffer), and these processes are relaxation-controlled. Ionic strength exerted a profound influence on the swelling of the microgels. Swelling was reversible and pulsatile with the changing environmental conditions. The pH-sensitive microgels were loaded with diltiazem hydrochloride and nifedipine (both antihypertensive drugs) and their release studies were performed in both the simulated gastric and intestinal pH conditions. The release was relatively quicker in pH 7.4 buffer than observed in 0.1 N HCl; the release followed non-Fickian transport in almost all the cases.

Glutaraldehyde crosslinked sodium alginate beads containing liquid pesticide for soil application

This paper presents experimental results on the successful encapsulation of a natural liquid pesticide neem (Azadirachta Indica A. Juss.) seed oil hereafter designated as NSO, using sodium alginate (Na-Alg) as a controlled release (CR) polymer after crosslinking with glutaraldehyde (GA). The NSO-containing beads have been prepared by changing the experimental variables such as the extent of crosslinking and the amount of loading in order to optimize the process variables. The absence of chemical interactions between active ingredients and polymer as well as crosslinking agent was confirmed by FTIR spectral measurements. The SEM data indicated that the structure of the walls of the beads are smooth and nonporous. The swelling results indicated that swelling of the polymeric beads decreases with increasing exposure time to the crosslinking agent. However, no significant variation in swelling was observed with different amounts of NSO loading. In order to understand the crosslinkability and its effect on the NSO release patterns of the beads, an attempt was made to calculate the molar mass between crosslinks using the Flory-Rehner equation. The release data have been fitted to an empirical equation to estimate the kinetic parameters.

In-vitro release kinetics of cefadroxil-loaded sodium alginate interpenetrating network beads.

This paper reports the development of new interpenetrating polymeric networks of sodium alginate with gelatin or egg albumin cross-linked with a common cross-linking agent, glutaraldehyde, for the in-vitro release of cefadroxil. The beads formed were characterized by Fourier transform infra-red spectroscopy, scanning electron microscopy and differential scanning calorimetry. Swelling/drying experiments were performed to compute the diffusion coefficients and the molecular mass between cross-links of the beads. The release results were evaluated using an empirical equation to understand the transport mechanism. The extent of cross-linking was studied in terms of the size and release characteristics of the beads. The experimental and derived quantities have been used to study their dependencies on the nature of the polymeric beads, transport mechanism, encapsulation efficiency and drug diffusion, as well as the cross-linking abilities of the polymers.

Hydrogels as controlled release devices in agriculture

Recently, there has been a great deal of research activity in the development of hydrogels as controlled release devices. The present review provides a brief introduction to various methods of synthesis, properties, types of hydrogels, and cross-linking agents which have been used for the preparation of hydrogels exhibiting suitable properties for agricultural applications.

Controlled release of diclofenac sodium from sodium alginate beads crosslinked with glutaraldehyde

Abstract Controlled release sodium alginate (Na–Alg) beads containing diclofenac sodium (DS) have been prepared by precipitation of Na–Alg in alcohol followed by crosslinking with glutaraldehyde (GA) in acidic medium. Preparation of the beads was optimized by considering the percentage entrapment efficiency, swelling capacity of beads in water and their release data. The percentage entrapment efficiency was found to vary between 30 and 71 depending upon the conditions of their preparations. The beads produced at higher temperatures and longer times of exposure to the crosslinking agent have shown the lower entrapment efficiency, but extended release of DS from the beads. The scanning electron microscopic studies indicated nonporous smooth surfaces and the differential scanning calorimetric data indicated the molecular level dispersion of the drugs in the beads.

Development of hollow microspheres as floating controlled-release systems for cardiovascular drugs : Preparation and release characteristics

Hollow microspheres of cellulose acetate loaded with four cardiovascular drugs (nifedipine [NFD], nicardapine hydrochloride [NCD], verapamil hydrochloride [VRP], and dipyridamole [DIP]) were prepared by a novel solvent diffusion-evaporation method. The oil-in-water emulsion prepared in an aqueous solution of 0.05% poly(vinyl alcohol) medium with ethyl acetate, a water-soluble and less toxic solvent, was used as the dispersing solvent. The yield of the microspheres was up to 80%. The microspheres had smooth surfaces, with free-flowing and good-packing properties. Scanning electron microscopy (SEM) confirmed their hollow structures, with sizes in the range 489–350 μm. The microspheres tended to float over the gastric media for more than 12 h. The drug loaded in hollow microspheres was in an amorphous state, as confirmed by differential scanning microscopy (DSC). The release of the drugs was controlled for more than 8 h. The release kinetics followed different transport mechanisms depending on the nature of the drug molecules.

MICROSPHERES AS FLOATING DRUG-DELIVERY SYSTEMS TO INCREASE GASTRIC RETENTION OF DRUGS

Gastric emptying is a complex process, which is highly variable and makes in vivo performance of the drug-delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 h. The floating or hydrodynamically controlled drug-delivery systems are useful in such applications. The present review addresses briefly the physiology of the gastric emptying process with respect to floating drug-delivery systems. In recent years, the multiparticulate drug-delivery systems are used in the oral delivery of drugs. One of the approaches toward this goal is to develop the floating microspheres so as to increase the gastric retention time. Such systems have more advantages over the single-unit dosage forms. The development of floating microspheres involves different solvent evaporation techniques to create the hollow inner core. The present review addresses the preparation and characterization of the floating microspheres for the peroral route of administration of the drug.

Encapsulation of antihypertensive drugs in cellulose-based matrix microspheres : characterization and release kinetics of microspheres and tableted microspheres

This study is an attempt to prepare microspheres loaded with two anti-hypertensive drugs viz., nifedipine (NFD) and verapamil hydrochloride (VRP) using cellulose-based polymers viz., ethyl cellulose (EC) and cellulose acetate (CA). Emulsification and solvent evaporation methods were optimized using ethyl acetate as a dispersing solvent. The particles are spherical in shape and have smooth surfaces, as evidenced by the scanning electron microscopy. The microspheres were characterized for their particle size and distribution, tapped density and encapsulation efficiency. Smaller sized particles with a narrow size distribution were produced with EC when compared to CA matrices. Molecular level drug distribution in the microspheres was confirmed by differential scanning calorimetry. The microspheres were directly compressed into tablets using different excipients. The drug release from CA was faster than EC microspheres and, also, the VRP release was faster than NFD. The excipients used in tableting showed an effect on the release as well as the physical properties of the tablets.This study is an attempt to prepare microspheres loaded with two antihypertensive drugs viz., nifedipine (NFD) and verapamil hydrochloride (VRP) using cellulose-based polymers viz., ethyl cellulose (EC) and cellulose acetate (CA). Emulsification and solvent evaporation methods were optimized using ethyl acetate as a dispersing solvent. The particles are spherical in shape and have smooth surfaces, as evidenced by the scanning electron microscopy. The microspheres were characterized for their particle size and distribution, tapped density and encapsulation efficiency. Smaller sized particles with a narrow size distribution were produced with EC when compared to CA matrices. Molecular level drug distribution in the microspheres was confirmed by differential scanning calorimetry. The microspheres were directly compressed into tablets using different excipients. The drug release from CA was faster than EC microspheres and, also, the VRP release was faster than NFD. The excipients used in tableting showed an effect on the release as well as the physical properties of the tablets.

A Review on Controlled Release of Nitrogen Fertilizers Through Polymeric Membrane Devices

Consequent to the better understanding of various agrochemicals, their functions during the growth cycles of plants and other aspects concerning economics, environment, and so forth, the controlled-release technology has emerged in the areas of fertilizers, herbicides, and pesticides. The present review discusses the technology and applications of controlled-release delivery systems concerning agrochemicals and the related technological advances with some critical suggestions. Emphasis is placed on inexpensive materials, simpler technologies, and statistical evaluation in planning and developing newer system. The interrelationship between technologies for controlled-release and membrane applications is discussed.