Faster Release Rate Research Articles

Development of dual–release pellets of the non-steroidal anti–inflammatory drug celecoxib

In the current study, once-a-day dual-release pellets of the selective non-steroidal anti-inflammatory drug celecoxib (200 mg) was developed to treat arthritis. Pellets were prepared where a 100 mg celecoxib, located in the outer layer, was released in an immediate-release (IR) pattern, whereas the remaining 100 mg celecoxib, located in the inner layer, was released in a sustained-release (SR) pattern. Pellets were subjected to four coating- and loading-stages using solid-dispersion and spray-drying including seal-coating, drug-loading, SR-coating, and IR-loading. Release studies were carried out using dissolution media with a pH range 1.2–12.0. The IR-stage showed a fast release rate, where 47.0% of celecoxib (equivalent to 94 mg) was released within the first hour. Whereas the SR-stage showed a sustained-release pattern up to 16 h. Celecoxib converted from crystalline to amorphous form during the development of pellets. This in turn improves the aqueous solubility and hence the dissolution of celecoxib. The results of stability studies showed that pellets were stable at 30 °C/65 %RH and 40 °C/75 %RH for 6 months. The present study demonstrated that celecoxib pellets can be an effective strategy for delivering the poorly-soluble drug celecoxib in a dual-release pattern.

Preparation of Quercetin Loaded Microparticles and their Antitumor Activity against Human Lung Cancer Cells (A549) in vitro

Novel quercetin-loaded microparticles (QM) were fabricated using coaxial electrospraying, characterized for surface morphology and release profile, and evaluated for antitumor activity in vitro. QM exhibited an average diameter of 1.69 ±1.13 mm, which was an appropriate size suitable for respiratory delivery. X-ray diffraction patterns showed that the components in QM existed in an amorphous physical form, leading to favorable interactions between the drug (quercetin), the polymer matrix (polyvinylpyrrolidone, PVP) and other excipients (sodium dodecyl sulfate and sucralose). QM performed much faster release rate compared with free quercetin powder (Q) in vitro. Furthermore, QM also showed more potent inhibitory effects on A549 cell growth with reduced cell viability, decreased cell migration and induced more G0/G1 phase cell cycle arrest than Q. Thus, the quercetin loaded microparticles exhibited more potent inhibitory effects than free quercetin on A549 cell. The increased antitumor activity could be attributed to the enhanced accumulation of quercetin in the A549 cells with the QM. However, further studies are necessary to elucidate the exact mechanisms.

A STUDY ON A NOVEL FORMULATION APPROACH TO DELIVER DOXYCYCLINE THROUGH BUCCAL ROUTE

Recent developments in drug delivery technologies have a great impact on the limitations of traditional oral drug delivery for both the pediatric and geriatric patients. Administration of drug via buccal mucosa is a modern alternative for overcoming low bioavailability, enzymatic inactivation and/or drug degradation in gastrointestinal tract, hence showing rapid onset of action. The aim of the study was to develop doxycycline (antibiotic) loaded buccal films for the treatment of a wide range of systemic and non-systemic bacterial and protozoa infections. The bases of each film were prepared using mucoadhesive polymers, plasticizer, cellulose gums, and instant release film former and penetration enhancer. Optimized films were characterized for weight, width. Length, thickness, surface pH, percentage swelling index, percentage elongation, percentage moisture content, percentage moisture uptake, hydration and in vitro drug release studies. Concentration of different polymers tailored the increase in release rate of doxycycline from the mucoadhesive buccal films. In conclusions, mucoadhesive buccal films can be a substitute route for the delivery of doxycycline as antibacterial or antiprotozoal drug with a faster release rate to reach the site of action.

Preparation and thermal properties of palmitic acid/expanded graphite/carbon fiber composite phase change materials for thermal energy storage

Using palmitic acid (PA), expanded graphite (EG), and carbon fiber (CF) as raw materials, PA/EG/CF composite phase change materials (CPCMs) with diverse CF contents were invented by melt blending approach. The effects of different ratios on thermal properties were studied by experimental characterization and testing. Scanning electron microscopy images displayed that PA was adsorbed in the pores of the EG surface, while CF was disorderly but uniformly embedded in the interior and surface of pores. The chemical stability and thermal decomposition stability of CPCM at low temperature were proved by Fourier transform infrared spectrometer and thermogravimetric analyzer results, respectively. According to the law of heat storage/release time and latent heat variation, the optimal ratio scheme was determined, and its heat storage/release time was 65% and 59% lower than pure PA, respectively. The form-stable materials were prepared by compression forming method, and thermal cycling experiment results demonstrated that the higher the content of CF, the stronger the inhibition of mass loss. Based on the experimental results, the PA/EG/CF CPCM has the advantages of stable phase transition, strong stability, and fast heat storage and release rate, so it has a marvelous application prospect in the field of low-temperature heat storage engineering.

ZnO and ZnO/CaO nanoparticles in alginate films. Synthesis, mechanical characterization, barrier properties and release kinetics

The aim of this paper was the synthesis of a nano-composed sodium alginate edible film containing ZnO and ZnO/CaO NPs and their mechanical, barrier and optical properties as well as the mechanism and release kinetics of the nanoparticles into food simulants were studied. ZnO NPs have a strong interaction with alginate molecules, reducing water vapour permeability and affecting their mechanical properties. On the other hand, ZnO/CaO NPs form aggregates that disrupt the polymeric structure of the alginate films increasing vapour permeability from 3.5 7.2 ± 0.3 g/Pa∗s∗m to 4.1 ± 0.1 g/Pa∗s∗m, and reducing the film's opacity from 14.2 ± 0.1 to 10.6 ± 0.2 Abs/mm. Also, the Ca and Zn release from the films into several food simulant media was studied, showing a Fickian type behaviour whit Peppas release coefficients (n) around 0.50 and faster release rates in lipophilic media, and that release kinetics are strongly dependent of the NPs concentration in the films. In conclusion, alginate edible films containing ZnO and ZnO/CaO can be used as active agents in the development of active food packaging.

Sustainable Dual Release of Antibiotic and Growth Factor from pH-Responsive Uniform Alginate Composite Microparticles to Enhance Wound Healing.

Hydrogel-based wound dressings provided a moist microenvironment and local release of bioactive molecules. Single drug loading along with fast release rates and usually in hydrogel sheets limited their performance. Hence, uniform alginate/CaCO3 composite microparticles (∼430 μm) with tunable compositions for sustainable release of drug and pH-sensitivity were successfully fabricated using microfluidic technology. Due to the presence of CaCO3 and the strong interactions with alginate molecules, lyophilized composite microparticles reverted to hydrogel state after rehydration. Regardless of microparticle states (hydrogel or lyophilized) and pH values (6.4 or 7.4), in vitro release rates of model drug were inversely related with CaCO3 concentrations and much lower than that for pure alginate microparticles. The release rate at pH 6.4 (simulating wound microenvironment) was always slower than that at pH 7.4 for the same type of microparticles. Rifamycin and basic fibroblast growth factor (bFGF) were independently encapsulated into AD-5-R and AD-40-F to achieve a fast release of rifamycin and a slower, more sustained release of bFGF, respectively; CD-F-R was a mixture of AD-5-R and AD-40-F at weight ratio 1/1. For AD-5-R and CD-F-R, inhibition zones of S. aureus were observed until day 5, showing a sustained antibacterial property. On the basis of in vitro wound healing model of NIH-3T3 cell micropattern on glass coverslips with a hole array, it was found that AD-40-F and CD-F-R significantly promoted cell proliferation and migration rates. In a full-thickness skin wound model of rats, CD-F-R microparticles significantly accelerated wound healing with higher granulation tissue thickness and better bioactivity to stimulate angiogenesis than the control group. Furthermore, CD-F-R microparticles demonstrated a good biocompatibility and biodegradability in vivo. Taken together, CD-F-R composite microparticles may ideally meet the requirements for different stages during wound healing and demonstrated a good potential to be used as dressing materials.

PH responsible and fluorescent Cy5.5-PEG-g-A-HA/CDDP complex nanoparticles: synthesis, characterization, and application for targeted drug delivery.

Clinical application of cisplatin (CDDP) against various solid tumors is often limited due to its poor selectivity and severe side effect. Considering this, in our study, CDDP was incorporated in fluorescent PEG amine grafted aldehyde hyaluronic acid by imine bond and metal ion coordination bond linking and formed a complex, the complex was then self-assembled into nanoparticles in water simply. FT-IR, XRD, DLS and SEM analysis demonstrated that the nanoparticles were prepared successfully and exhibited a spherical structure with size ranged from 216.4 to 372.3 nm in diameter. CDDP releasing from the nanoparticles was in a controlled manner, and had faster release rate at lower pH, indicating the nanoparticles were responsive to tumor micro-acid environment. Since fluorescent Cy5.5 and targeting hyaluronic acid existed on the surface of the nanoparticles, CLSM images clearly showed that the nanoparticles could target and internalize into HeLa cells, and then inhibited the growth of HeLa cells. In addition, MTT, AO-EB staining, and hemolysis assay showed that the nanoparticles had good cyto-/hemo-compatibility. Hence, the nanoparticles had the potential to be used for cancer therapy and diagnosis. The further in vivo experiment will be shown in the next work. pH responsible and fluorescent Cy5.5-PEG-g-A-HA/CDDP complex nanoparticles were facilely fabricated for controlled and targeted delivery of CDDP.

Effect of Adjuvant Release Rate on the Immunogenicity of Nanoparticle-Based Vaccines: A Case Study with a Nanoparticle-Based Nicotine Vaccine.

Adjuvants are a critical component for vaccines, especially for a poorly immunogenic antigen, such as nicotine. However, the impact of adjuvant release rate from a vaccine formulation on its immunogenicity has not been well illustrated. In this study, we fabricated a series of hybrid-nanoparticle-based nicotine vaccines to study the impact of adjuvant release rate on their immunological efficacy. It was found that the nanovaccine with a medium or slow adjuvant release rate induced a significantly higher anti-nicotine antibody titer than that with a fast release rate. Furthermore, the medium and slow adjuvant release rates resulted in a significantly lower brain nicotine concentration than the fast release rate after nicotine challenge. All findings suggest that adjuvant release rate affects the immunological efficacy of nanoparticle-based nicotine vaccines, providing a potential strategy to rationally designing vaccine formulations against psychoactive drugs or even other antigens. The hybrid-nanoparticle-based nicotine vaccine with an optimized adjuvant release rate can be a promising next-generation immunotherapeutic candidate against nicotine.

Experimental assessment of the utilization of a novel interpenetrating polymer network in different processes in the agricultural sector

ABSTRACTWe synthesized a biodegradable, controlled release formulation via the impregnation of methyl methacrylic acid onto the natural polysaccharide, gum tragacanth, and a polyacrlyic‐based hydrogel with glutaraldehyde as crosslinker. The biodegradation behavior of the prepared interpenetrating polymer network (IPN) was investigated with soil burial and composting methods, and the biodegradability stages were studied with Fourier transform infrared spectroscopy and scanning electron microscopy analyses. The controlled release data of the calcium nitrate was analyzed in accordance with Fick's power law, and the kinetics parameters of the release process were calculated. The values of the initial and lateral diffusion coefficients indicated a fast initial release rate of the fertilizers in comparison to the lateral release. The synthesized IPN was degraded 91.62% within 11 weeks under composting methods, whereas it degraded 78.83% under the soil burial method. The results show that the synthesized IPN was ecofriendly and could be used for the controlled release of agrochemicals. The impact of the degraded IPN on the fertility of the soil was also studied. We concluded from the results obtained that the biodegraded IPN did not have any adverse effects on the soil fertility. Hence, this biodegradable IPN could be of great significance from a green revolution point of view. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019, 136, 47739.

Effect of dose and release rate of CTGF and TGFβ3 on avascular meniscus healing.

Meniscus tears in the avascular region rarely functionally heal due to poor intrinsic healing capacity, frequently resulting in tear propagation, followed by meniscus deterioration. Recently, we have reported that time-controlled application of connective tissue growth factor (CTGF) and transforming tissue growth factor β3 (TGFβ3) significantly improved healing of avascular meniscus tears by inducing recruitment and step-wise fibrocartilaginous differentiation of mesenchymal stem/progenitor cells (MSCs). In this study, we investigated effects of the dose of CTGF and the release rate of TGFβ3 on avascular meniscus healing in our existing explant model. Our hypothesis was that dose and release rate of CTGF and TGFβ3 are contributing factors for functional outcome in avascular meniscus healing by stem cell recruitment. Low (100 ng/ml) and high (1,000 ng/ml) doses of CTGF as well as fast (0.46 ± 0.2 ng/day) and slow (0.29 ± 0.1 ng/day) release rates of TGFβ3 were applied to our established meniscus explant model for meniscus tears in the inner-third avascular region. The release rate of TGFβ3 was controlled by varying compositions of poly(lactic-co-glycolic acids) (PLGA) microspheres. The meniscus explants were then cultured for 8 weeks on top of mesenchymal stem/progenitor cells (MSCs). Among the tested combinations, we found that a high CTGF dose and slow TGFβ3 release are most effective for integrated healing of avascular meniscus, demonstrating improvements in alignment of collagen fibers, fibrocartilaginous matrix elaboration and mechanical properties. This study may represent an important step toward the development of a regenerative therapy to improve healing of avascular meniscus tears by stem cell recruitment. © 2019 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 37:1555-1562, 2019.

Encapsulation of metronidazole in polycaprolactone microspheres

Non-aqueous oil-in-oil solvent evaporation technique is used for the preparation of polycaprolactone microspheres loaded with the antibiotic metronidazole by introducing different masses for the drug. The prepared microspheres are characterized by calculating drug encapsulation and drug loading percentages, measuring the corresponding particle size, performing FT-IR polymer-drug compatibility study and in vitro drug release. Moderate drug encapsulation values with a maximum of 34% are observed due to the low molecular weight of the drug. Microspheres had a particle size ranging between 130 and 280 µm with a spherical profile and porous structure. FT-IR study showed no interactions between the drug and the polymer. Drug release studies showed fast release rates for all the formulations with the slowest release for the highest drug loading.
 Keywords: polycaprolactone, metronidazole, targeted drug delivery, solvent evaporation.

Ignition sensitivity of different compositional wood pellets and particle size dependence

Partial or complete substitution of coal with renewable biomass like wood is a sustainable and effective solution to reduce the CO2 emissions in the atmosphere. Utilization of these woods in the form of compact pellets facilitates in its handling and transportation with higher energy density. However, for electric power generation the pellets are broken up into their constituent milled finer particles for burning as a pulverised biomass flame. There is a dust fire/explosibility hazards in the process handling facilities such as in storage, conveying and milling. In the present work, four commercial pellets were investigated, and each pellet sample was split into three size ranges <63 μm, 63–500 μm and <500 μm. The flame propagation characteristics and their lean flammability limit for each pulverised pellet was determined using modified Hartmann dust explosion tube. It was found that the fine particles, with lower lean flammability limits of 0.3–0.7 equivalence ratio, intensify the explosibility risk (dP/dt of 10–15 bar/s for most reactive concentration) of the dust due to fast volatile release rate. Comparison was also made between particle size distribution (PSD) of the finer fractions (<63 μm) of wood samples in comparison to crop residue samples that showed 70–80% larger size distribution for wood samples due to elongated particles as showed by Scanning Electron Microscope (SEM). Results showed that the ash + moisture content had a stronger effect on wood samples than on agricultural residue's samples. The results showed that the explosibility characteristics of the pellets industry's feed-stocks was variable and dependent on the pellet composition and this needs to be taken into account in explosion protection and in utilising the pellets in the main pulverised biomass combustion.

APPLICATION OF LIQUISOLID TECHNOLOGY TO ENHANCE THE DISSOLUTION OF CEFIXIME FROM ITS ORAL CAPSULES

Objective: Oral drug delivery is the most desired route for drug administration for its well-known features. Therefore, many attempts were implemented to improve the poor solubility of many active ingredients in order to enhance their dissolution and absorption via the oral route. From these, the liquisolid system is a very promising technology for enhancing solubility and bioavailability of poorly soluble drugs.Methods: In this research, oral capsules of cefixime were prepared by liquisolid technique after mixing different concentrations of the drug with propylene glycol (non-volatile solvent), followed by their addition to different proportions of microcrystalline cellulose and aerosil i.e. different carrier: coating (R-value). The liquisolid capsules were evaluated for In vitro disintegration and dissolution in addition to content uniformity and weight variations. Furthermore, solubility studies, scanning electron microscope (SEM) were performed to the optimum formula. Finally, the release profile of the optimum formula was compared with the marketed cefixime capsules.Results: Liquisolid formula (F3) with 70% cefixime and R-value equals 10 was selected as the optimum formula having higher % release in 45 min (99.5%±0.53) compared to other formulas with faster release rate in the first 20 min than marketed capsules. It had an acceptable disintegration time (25 min±0.76), content uniformity (197.6±0.92) and weight variation (698.04±0.16). Results of solubility study, SEM assured enhancement in solubility and dispersibility of the drug.Conclusion: This research proved that liquisolid system is a promising technology in improving the solubility and dissolution of cefixime from its capsules and hence it may improve its absorption and oral bioavailability.

Pyraclostrobin-loaded poly (lactic-co-glycolic acid) nanospheres: Preparation and characteristics

We used poly (lactic-co-glycolic acid) (PLGA) as a carrier polymer for pyraclostrobin-loaded nanospheres. Using the ultrasound emulsification-solvent evaporation method, the physicochemical characteristics and release properties of the pyraclostrobin-loaded nanospheres were studied by dialysis. The optimal nanospheres prepared had a diameter of 0.6 μm, an active ingredient loading of 17.2%, and a loading rate of 89.7%. Infrared spectroscopy data and differential scanning calorimetry revealed that pyraclostrobin was successfully embedded in the carrier PLGA, and photostability tests indicated enhanced ultraviolet resistance of pyraclostrobin-loaded PLGA nanospheres nanospheres. Release property testing indicated that smaller particles had a faster release rate. Nanospheres also had a faster release rate in slightly acidic and slightly basic environments than in a neutral condition. Agitated nanospheres had a faster release rate than immobile nanospheres. The cumulative release kinetics of pyraclostrobin-loaded nanospheres was consistent with the first order kinetic equation and the Weibull equation.

Effect of Binary Organic Solvents Together with Emulsifier on Particle Size and In vitro Behavior of Paclitaxel-Encapsulated Polymeric Lipid Nanoparticles.

Biodegradable nanoparticles with diameters between 100 nm and 500 nm are of great interest in the contexts of targeted delivery. The present work provides a review concerning the effect of binary organic solvents together with emulsifier on particle size as well as the influence of particle size on the in vitro drug release and uptake behavior. The polymeric lipid nanoparticles (PLNs) with different particle sizes were prepared by using binary solvent dispersion method. Various formulation parameters such as binary organic solvent composition and emulsifier types were evaluated on the basis of their effects on particle size and size distribution. PLNs had a strong dependency on the surface tension, intrinsic viscosity and volatilization rate of binary organic solvents and the hydrophilicity/hydrophobicity of emulsifiers. Acetone-methanol system together with pluronic F68 as emulsifier was proved to obtain the smallest particle size. Then the PLNs with different particle sizes were used to investigate how particle size at nanoscale affects interacted with tumor cells. As particle size got smaller, cellular uptake increased in tumor cells and PLNs with particle size of ~120 nm had the highest cellular uptake and fastest release rate. The paclitaxel (PTX)-loaded PLNs showed a size-dependent inhibition of tumor cell growth, which was commonly influenced by cellular uptake and PTX release. The PLNs would provide a useful means to further elucidate roles of particle size on delivery system of hydrophobic drugs.

Bioengineering the spider silk sequence to modify its affinity for drugs.

BackgroundSilk is a biocompatible and biodegradable material, able to self-assemble into different morphological structures. Silk structures may be used for many biomedical applications, including carriers for drug delivery. The authors designed a new bioengineered spider silk protein, EMS2, and examined its property as a carrier of chemotherapeutics.Materials and methodsTo obtain EMS protein, the MS2 silk monomer (that was based on the MaSp2 spidroin of Nephila clavipes) was modified by the addition of a glutamic acid residue. Both bioengineered silks were produced in an Escherichia coli expression system and purified by thermal method. The silk spheres were produced by mixing with potassium phosphate buffer. The physical properties of the particles were characterized using scanning electron microscopy, atomic force microscopy, Fourier-transform infrared spectroscopy, and zeta potential measurements. The MTT assay was used to examine the cytotoxicity of spheres. The loading and release profiles of drugs were studied spectrophotometrically.ResultsThe bioengineered silk variant, EMS2, was constructed, produced, and purified. The EMS2 silk retained the self-assembly property and formed spheres. The spheres made of EMS2 and MS2 silks were not cytotoxic and had a similar secondary structure content but differed in morphology and zeta potential values; EMS2 particles were more negatively charged than MS2 particles. Independently of the loading method (pre- or post-loading), the loading of drugs into EMS2 spheres was more efficient than the loading into MS2 spheres. The advantageous loading efficiency and release rate made EMS2 spheres a good choice to deliver neutral etoposide (ETP). Despite the high loading efficiency of positively charged mitoxantrone (MTX) into EMS2 particles, the fast release rate made EMS2 unsuitable for the delivery of this drug. A faster release rate from EMS2 particles compared to MS2 particles was observed for positively charged doxorubicin (DOX).ConclusionBy modifying its sequence, silk affinity for drugs can be controlled.

Mechanisms of enhanced antiglioma efficacy of polysorbate 80-modified paclitaxel-loaded PLGA nanoparticles by focused ultrasound.

The presence of blood‐brain barrier (BBB) greatly limits the availability of drugs and their efficacy against glioma. Focused ultrasound (FUS) can induce transient and local BBB opening for enhanced drug delivery. Here, we developed polysorbate 80‐modified paclitaxel‐loaded PLGA nanoparticles (PS‐80‐PTX‐NPs, PPNP) and examined the enhanced local delivery into the brain for glioma treatment by combining with FUS. Our result showed PPNP had good stability, fast drug release rate and significant toxicity to glioma cells. Combined with FUS, PPNP showed a stronger BBB permeation efficiency both in the in vitro and in vivo BBB models. Mechanism studies revealed the disrupted tight junction, reduced P‐glycoprotein expression and ApoE‐dependent PS‐80 permeation collectively contribute to the enhanced drug delivery, resulting in significantly stronger antitumour efficacy and longer survival time in the tumour‐bearing mice. Our study provided a new strategy to efficiently and locally deliver drugs into the brain to treat glioma.

Two-stage controlled release system possesses excellent initial and long-term efficacy.

In this work, a series of polyurea-based lambda-cyhalothrin-loaded microcapsules (MCs) with three different size distributions (average diameters of 1.35 μm, MC-S; 5.13 μm, MC-M; and 21.48 μm, MC-L) were prepared and characterized. The results indicated that MCs with a smaller particle size distribution had a faster release rate and excellent initial efficacy against pests. MC-L had a remarkably slow incipient release rate, outstanding photostability and better later-stage efficacy than that of the other tested MCs. The results clarified that the diameter distribution of MCs is the key factor in determining the release property and bioactivity of the MC formulations. Subsequently, the binary mixture MC formulations of MC(+M), MC(S+L) and MC(M+L) were obtained by mixing MC-S, MC-M or MC-L at 1:1 to establish a two-stage release system utilized for foliar application situations. Greenhouse and field experiments showed that MC(S+L) provided an optimal efficacy, and its effective duration was much longer than that of the emulsifiable concentrate (EC) group. Therefore, the release system established in this study was simple and workable for regulating the initial and long-term efficacy by adjusting the particle size distribution; in addition, this system has potential applications in other fields such as drug delivery devices.

Synthesis and evaluation of water soluble pH sensitive poly (vinyl alcohol)-doxorubicin conjugates

The accuracy of spatiotemporal control cargo delivery and release are primordial to enhance the therapeutic efficiency and decrease the undesirable effects, in this context a novel prodrug were developed based on biocompatible polyvinyl alcohol (PVA) substrate. PVA was conjugated to doxorubicin (PVA-DOX) via an acid-labile hydrazone linkage. PVA was first functionalized with acidic groups, then reacted with hydrazine hydrate to form an amide bond. The amine group of PVA hydrazide was linked to carbonyl group (C = O) of DOX to form a pH sensitive hydrazone bond. The molecular structure of the PVA-DOX was confirmed by FTIR, XPS, and 1H-NMR analysis methods. The degree of grafting were evaluated by TGA and confirmed by XPS, which reveals the successful bond attachment of DOX to PVA. Our findings confirm pH dependent DOX release from PVA-DOX prodrug with faster release rate in acidic environment (pH 5.0, pH 6.0) and slower release rate in neutral pH environment (pH 7.4). Compared to the primary DOX, our synthesized PVA-DOX conjugates could exhibit a promising therapeutic effect, high biocompatibility and zero premature release. The results prove the successful synthesis of PVA-DOX conjugates with high efficiency.

FORMULATION EVALUATION AND OPTIMIZATION OF ORODISPERSIBLE TABLETS OF PANTOPRAZOLE SODIUM BY THE USING OF DIFFERENT SUPERDISINTEGRANTS

Objective: The objective of this study was to formulate and optimize an orodispersible formulation of pantoprazole sodium using a 32 factorial design for optimized the superdisintegrant concentration. Methods: Various concentrations (2%, 4%, and 6%) of superdisintegrants (sodium starch glycollate [SSG] and crospovidone [CP]) were added in the formulation, all processing steps are carried out at a temperature below 250c and relative humidity &lt;35%. Procedure to manufacture orodispersible tablets by direct compression was established. Results: The results show that the presence of a superdisintegrants is desirable for orodispersion. The best-optimized batch found was the batch having amount of CP 4.37 mg and SSG 10.59 mg. All the formulations satisfied the limits of orodispersion with a dispersion time of &lt;30 s best formulation showed a disintegration time (DT) of 30 s, % friability is 0.82%, drug content of 96– 99.4, and fast drug release rate of 80 % of drug release within 10 min. Conclusion: The optimized batch was evaluated for thickness, weight variation, hardness, friability, DT dissolution, and accelerated stability study for a period of 3 months. The similarity factor was calculated for comparison of dissolution profile before and after stability studies. The f2 value was found more than 50 that indicate a good similarity between both the dissolution profiles. Hence, the results of stability studies reveal that the developed formulation has good stability.