Extrusion Spheronization Research Articles

Enhanced bioavailability and efficacy in antimalarial treatment through QbD approach enteric encased inclusion delivery.

Aim: In this study, we aimed to prepare enteric encapsulated spheroids containing inclusion complex using quality by design approach.Methods: A Box-Behnken design was employed to determine effects of variables on selected responses. Risk assessment was conducted using Ishikawa fishbone diagram. A model with a p-value was less than 0.5 for being a significant error of model was determined based on significance 'lack of fit' value. Spheroids were formulated using the extrusion spheronization technique and were characterized using analytical techniques.Results: In vitro release was performed in both acidic (pH 1.2) and simulated intestinal (pH 6.8) conditions. Permeability studies demonstrated tenfold enhancement compared with arteether. In vivo studies further validated increase of 51.8% oral bioavailability. Exvivo studies revealed 3.4-fold enhancement in antimalarial activity compared with arteether.Conclusion: These findings highlight effectiveness of inclusion complexation technique as a viable approach to enhance solubility and bioavailability for drugs with low aqueous solubility.

Croscarmellose Sodium as Pelletization Aid in Extrusion-Spheronization

Only few excipients are known to be suitable as pelletization aids. In this study, the potential use of croscarmellose sodium (CCS) as pelletization aid was investigated. Furthermore, the impact of cations on extrusion-spheronization (ES) of CCS was studied and different grades of CCS were tested. The influence of different cations on the swelling of CCS was investigated by laser diffraction. Mixtures of CCS with lactose monohydrate as filler with or without the inclusion of different cations were produced. The mixtures were investigated by mixer torque rheometry and consequently extruded and spheronized. Resulting pellets were analyzed by dynamic image analysis. In addition, mixtures of different CCS grades with dibasic calcium phosphate anhydrous (DP) and a mixture with praziquantel (PZQ) as filler were investigated. Calcium and magnesium cations caused a decrease of the swelling of CCS and influenced the use of CCS as pelletization aid since they needed to be included for successful ES. Aluminum, however, led to an aggregation of the CCS particles and to failure of extrusion. The inclusion of cations decreased the uptake of water by the mixtures which also reduced the liquid-to-solid-ratio (L/S) for successful ES. This was shown to be dependent on the amount of divalent cations in the mixture. With DP or PZQ as filler, no addition of cations was necessary for a successful production of pellets, however the optimal L/S for ES was dependent on the CCS grade used. In conclusion, CCS can be used as a pelletization aid.Graphical

Investigation of the Electrokinetic Potential of Granules and Optimization of the Pelletization Method Using the Quality by Design Approach.

The preparation of pellets using a high-shear granulator in a rapid single-step is considered a good economic alternative to the extrusion spheronization process. As process parameters and material attributes greatly affect pellet qualities, successful process optimization plays a vital role in producing pellet dosage forms with the required critical quality attributes. This study was aimed at the development and optimization of the pelletization technique with the Pro-CepT granulator. According to the quality by design (QbD) and screening design results, chopper speed, the volume of the granulating liquid, binder amount, and impeller speed were selected as the highest risk variables for a two-level full factorial design and central composite design, which were applied to the formula of microcrystalline cellulose, mannitol, and with a binding aqueous polyvinylpyrrolidone solution. The design space was estimated based on physical response results, including the total yield of the required size, hardness, and aspect ratio. The optimized point was tested with two different types of active ingredients. Amlodipine and hydrochlorothiazide were selected as model drugs and were loaded into an optimized formulation. The kinetics of the release of the active agent was examined and found that the results show a correlation with the electrokinetic potential because amlodipine besylate can be adsorbed on the surface of the MCC, while hydrochlorothiazide less so; therefore, in this case, the release of the active agent increases. The research results revealed no significant differences between plain and model drug pellets, except for hydrochlorothiazide yield percent, in addition to acceptable content uniformity and dissolution enhancement.

Formulation and optimization of a single-layer coat for targeting budesonide pellets to the descending Colon

The current budesonide formulations are inadequate for addressing left-sided colitis, and patients might hesitate to use an enema for a prolonged time. This study focuses on developing a single-layer coating for budesonide pellets targeting the descending colon. Pellets containing budesonide (1.5%w/w), PVP K30 (5%w/w), lactose monohydrate (25%w/w) and Avicel pH 102 (68.5%w/w) were prepared using extrusion spheronization technique. Coating formulations were designed using response surface methodology with pH and time-dependent Eudragits. Dissolution tests were conducted at different pH levels (1.2, 6.5, 6.8, and 7.2). Optimal coating formulation, considering coating level and the Eudragit (S + L) ratio to the total coating weight, was determined. Budesonide pellets were coated with the optimized composition and subjected to continuous dissolution testing simulating the gastrointestinal tract. The coating, with 48% S, 12% L, and 40% RS at a 10% coating level, demonstrated superior budesonide delivery to the descending colon. Coated pellets had a spherical shape with a uniform 30 µm thickness coating, exhibiting pH and time-dependent release. Notably, zero-order release kinetics was observed for the last 9 h in colonic conditions. The study suggests that an optimized single-layer coating, incorporating pH and time-dependent polymers, holds promise for consistently delivering budesonide to the descending colon.

FORMULATION AND DEVELOPMENT OF BIOADHESIVE PELLETS FOR MANAGEMENT OF HELICOBACTER PYLORI INFECTION

Helicobacter pylori, a gram-negative bacterium, is a group I carcinogen which is responsible for duodenal ulcer, gastric ulcer, and gastric cancer. The existing treatment is based on the use of proton pump inhibitors, but is inadequate owing to factors such as low concentration of drug reaching the target site, short residence time, and resistance to activity. Intending to mitigate these limitations, bioadhesive pellets of tinidazole and pantoprazole sodium sesquihydrate for the management of H. pylori infection were developed. Tinidazole-loaded pellets will act on gastric mucosa and pantoprazole-loaded pellets will release the drug in the intestine. Readily dispersible bioadhesive pellets were formulated by extrusion spheronization using Noveon® AA and hydroxypropyl methyl cellulose (HPMC) as the matrix-forming polymers and microcrystalline cellulose as the core-forming agent. The size of placebo pellets was 1.192±0.017mm. Pantoprazole pellets were coated with Eudragit® S100 to achieve sustained drug release in the intestine. In vitro release studies of pellets showed that 98.331±0.456% and 99.438±0.465% of tinidazole and pantoprazole, respectively were released by the end of 8 h. Ex vivo mucoadhesion study on the gastric mucosa of goat demonstrated a mucoadhesive force of 2.3544±0.02 N. The study thus indicates that the developed formulation sustains the release of tinidazole as well as pantoprazole sodium and could prove to be efficacious and promising for H. pylori eradication at lower doses, reduced adverse effects, and enhanced bioavailability.

TECHNIQUES AND EVALUATION TESTS FOR COLON CANCER TREATMENT USING PELLETS: A REVIEW

This review outlines the manufacturing process for globular pellets. The production method includes the following steps: drug stacking, displacement-merumerization, cryopelletization, shrink, balling, hot-soften extrusion generation, freeze pelletization, spray-drying, and spray-congealing. The benefits and risks of several pelletization methods were discussed. The current study's objective is to examine the efficacy of anticancer drugs and metal chelators in treating colorectal cancer (CRC). Phytic acid, 5-fluorouracil (5-FU), microcrystalline cellulose (MCC) PH 100 and 1 compile in the pellets, hydroxypropyl methylcellulose (HPMC), and barium sulphate were processed utilizing the extrusion spheronization technology. To achieve colon-specific medication delivery, Eudragit S100 was layered over the ability pellets. Pellets have been praised for a variety of micromeritic and medicinal qualities. In the Ehrlich ascites carcinoma (EAC)-driven patient-derived zenograft (PDX) paradigm, the in vivo treatment potency separates the pharmacokinetic and pharmacodynamic bounds. By chelating manganese, phytic acid, and five-FU combinations, they appear to provide more cytotoxic interest through a better reactive oxygen species (ROS) stage. Later pharmacokinetic studies showed a maximum 50% drop in Cmax within the finished setup, indicating decreased inherent exposure to the drug component. KEYWORDS: Pelletization, Merumerization, Drying, cancer, Spheronization, colorectal cancer.

Design, Synthesis, Evaluation, and Molecular Docking Study of Ascorbic Acid Dual-Coated Omeprazole Pellets and the Antioxidative Effect of Ascorbic Acid on Omeprazole-Induced Renal Injury in an Animal Model.

The present study was carried out to investigate the antioxidant effect of ascorbic acid on omeprazole (O.P.)-induced acute kidney infection (AKI). Design of experiment (DoE) was employed to fabricate formulations (P1-P8) by the extrusion spheronization technique, and they were evaluated using various analytical techniques. P1-P8 formulations have % drug loading ranging from 56.34 ± 1.10 to 98.67 ± 1.05%, encapsulation efficiency from 70.98 ± 0.96 to 98.67 ± 1.05%, percentage drug release varying from 36.56 ± 1.34 to 93.45 ± 1.45%, Hausner's ratio ranging from 1.026 ± 0.05 to 1.065 ± 0.02%, and Carr's index varying from 2.3 ± 0.07 to 6.1 ± 0.06 g/mL. The optimized formulation (P6) was dual-coated with Eudragit L-100 (5% w/v) and ascorbic acid (2% w/v). A smooth uniform morphology was found after coating, and particle size nonsignificantly changed from 85.31 ± 77.43 to 101.99 ± 65.56 μm. IR spectra showed omeprazole characteristic peaks confirming drug loading, and peaks at 1747.40 and 1611.51 cm-1 confirmed ascorbic acid and Eudragit L-100 coating. X-ray diffraction (XRD) analysis confirmed the crystalline nature, and thermal degradation studies until 500 °C demonstrated increased stability after coating. Cytotoxicity analysis with 97% cell viability revealed the nontoxic behavior of pellets. In vitro dissolution studies of coated pellets showed <20% drug release at pH 1.2 and 99.54% at pH 6.8. Animal studies showed that pure omeprazole showed a nonsignificant decrease in weight, urine output, and fecal output compared to rodents on ascorbic acid pellets. Increased uric acid and creatinine levels in the group on pure omeprazole indicated AKI. Histopathological studies of renal cells also supported these results. The integration of experimental pellet formulation with molecular docking simulations has unveiled the potential of ascorbic acid and omeprazole as highly promising therapeutic agents for addressing oxidative stress and inflammation.

Influence of Extrudate-Based Textural Properties on Pellet Molding Quality.

As the precursor of pellets, the extrudate has a direct impact on the molding quality of the pellets. Therefore, the correlation between the surface roughness of the extrudates and the molding quality of pellets with pure microcrystalline cellulose (MCC) formulations and those containing traditional Chinese medicine (TCM) formulations was explored. MCC was used as a pelleting agent, mixer torque rheometry (MTR) was used to guide the optimal dosage of the wetting agent, and TCM extracts (drug loadings of 20% to 40%) were selected as model drugs to prepare the extrudates and pellets under the same extrusion spheronization process conditions. The surface roughness and texture parameters of extrudates were analyzed via a microscope and texture analyzer, respectively, and the quality of pellets was evaluated. The extrudate roughness of the pure MCC prescription decreased and then increased with increasing water addition, while the extrudate roughness of the prescription containing TCM extracts tended to increase and then decrease. The addition of water affected the extrudate properties, with TCM extract molecules filling gaps in the MCC structure, leading to rough surfaces. The extrudate roughness of the TCM prescriptions was significantly greater than that of the pure MCC prescriptions at optimal water addition levels, resulting in ideal pellets.

Experimental and kinetic study on the cyclic removal of low concentration CO2 by amine adsorbents in confined spaces

Amine-based adsorbents show great promise for removing low-concentration CO2 from environmental control and life support systems (ECLSSs) to ensure crew safety and task execution. In this work, granular silica gel (SG) support was prepared by the extrusion–spheronization (ES) method, and amine-based adsorbent pellets were synthesized by impregnating the SG support with tetraethylenepentamine (TEPA). Dynamic CO2 circulation removal tests were carried out under simulated confined space conditions in a 100 L chamber to evaluate the low concentration CO2 removal performance of the adsorbent pellets. The effect of operating parameters on CO2 removal performance was investigated by orthogonal experiments. CO2 adsorption capacity and removal efficiency were significantly affected by CO2 concentration and reaction temperature, while reaction rate was intimately depended on CO2 concentration and gas flow rate. The maximum CO2 adsorption capacity (0.55 mmol CO2/g), removal efficiency (83.25%) and reaction rate (0.93 mmol CO2/min) were achieved under the optimized conditions of 20 °C, 1.25%CO2 and 2 L/min. A kinetic equation well representing the correlation between reaction rate and CO2 concentration and gas flow rate was established. The TEPA-SG-ES adsorbent pellets exhibited satisfactory working stability, with CO2 removal efficiency and adsorption capacity slightly decreased from 83.25% and 0.55 mmol CO2/g to 75.45% and 0.53 mmol CO2/g in 10 cycles, respectively. The slight decay in CO2 adsorption performance was associated with the oxidative degradation of amine species in oxygenated atmosphere to form amide, nitrite and imine phases, and the change of amine distribution over the pellets in multiple cycles. Overall, the desired TEPA-SG-ES adsorbent pellets could be nice scavenger candidates for circulating purification of CO2 in confined spaces.

Green Tea Extract Solid Dispersion Pellets with Enhanced Permeability for Hyperlipidemia

Green tea extract, rich in polyphenols like catechins, has been reported to have pharmacological benefits in patients with hyperlipidemia. The minimal membrane permeability of green tea limits its use in terms of bioavailability. To improve the permeability of green tea catechins in order to enhance theiranti-hyperlipidemia activity, a surfactant-based polymer was used to formulate a solid dispersion of green tea and convert it into commercially acceptable pellets. Green tea extract solid dispersions (GTE-SDs) were prepared withsolvent evaporation method using Soluplus® as a carrier. The GTE-SDs were evaluated for ex vivo permeation studies and characterized using FTIR, DSC, and XRD for confirming the formation of SD. The GTE-SDs exhibiting enhanced ex vivo permeation of EGCG were converted into a pellet formulation using the extrusion spheronization technique while being optimized using a 32 full factorial design. Soluplus® exhibited a four-fold improvement in the ex vivo permeation of EGCG from GTE-SD pellets (33.27%) as compared to GTE (10.43%) (p-value &lt; 0.0001). In male Wistar rats, optimized GTE-SD pellets reduced the lipid blood profiles as compared to GTE (p-value &lt; 0.0001). Thus, GTE-SD pellets can serve as an effective drug delivery platform for hyperlipidemia.

One‐step fabrication of Li2TiO3 ceramic pebbles using pulsed YAG laser

AbstractA large amount of Li‐containing ceramic breeder pebbles is packed in the solid breeding blanket of a nuclear fusion reactor. Several pebble fabrication technologies have been proposed in previous studies, including wet process, emulsion method, extrusion spheronization, additive manufacturing, and melt process. However, a simple, energy‐effective, and scalable fabrication technology remains to be developed for the automated mass production and reprocessing of used radioactive pebbles post‐operation. Selective laser melting potentially enables the quick and automated fabrication of breeder pebbles. Herein, we employ a high‐power density pulse laser to produce ceramic breeder pebbles. A pulsed YAG laser was irradiated over a lithium metatitanate (Li2TiO3) powder bed in air, and the corresponding temperature was monitored using fiber‐type infrared pyrometers. Spherical Li2TiO3 pebbles were successfully fabricated in a single step with an average diameter of 0.78 ± 0.13 μm and the sintering density of 87.4% ± 5.6% (input power: 7.9 J/pulse). The irradiated Li2TiO3 powder melted and turned spherical under surface tension and rapidly solidified, resulting in uniaxial fine grains and a decrease in the degree of long‐range cation ordering.

Facile fabrication of silica aerogel supported amine adsorbent pellets for Low-concentration CO2 removal from confined spaces

Amine-based adsorbents show promise for removing low-concentration CO2 from environmental control and life support systems (ECLSSs), while the powder adsorbents are facing the challenges of reaction non-uniformity, pressure drop and material elutriation. To solve the problems, amine-based adsorbent pellets are fabricated by the extrusion–spheronization (ES), agar-assisted moulding (AM) and graphite-casting (GC) methods. The adsorbent pellets are further modified with pore-forming template for improved CO2 adsorption performance. The influences of granulation and pore-forming template modification on the structure-performance relationships of the adsorbent pellets are investigated. Granulation exerts adverse effect on the pore structure of tetraethylenepentamine supported on silica gel (TEPA-SG) adsorbent, which is not conducive to the bulk diffusion of CO2, and the CO2 adsorption capacity and kinetics thus have been impaired. The TEPA-SG-ES adsorbent pellets prepared by the extrusion–spheronization method show a relatively higher CO2 capture capacity of 1.01 mmol CO2/g due to better textural parameters and uniform dispersion of amine species. Thanks to the extrusion process, the adsorbent pellets also exhibit good mechanical properties with a high compressive strength of 10.90 MPa and low abrasion index of 0.36%. Both the textural properties and CO2 uptakes of the pellets can be restored upon template modification, and the promoting effect depends on the different templates employed due to their distinct pyrolysis rates and pathways. Mechanical properties will be adversely affected by the doped pore-forming template. The TEPA-SG-ES-UA pellets prepared with urea modification exhibit a great CO2 capture capacity of 1.48 mmol CO2/g and good mechanical properties with a high compressive strength of 4.90 MPa and a low abrasion index of 0.87%, and it could be a nice adsorbent candidate for removing low-concentration CO2 from ECLSSs.

Bio-adsorbent hydroxyapatite for drinking water defluoridation: column performance modelling studies.

Waste marble powder (WMP) is a rich source of calcium and magnesium salts having an affinity for fluoride ions and therefore serves as a good defluoridation agent. Hydroxyapatite was synthesized from WMP generated by the marble processing industry to make an adsorbent for drinking water defluoridation. The synthesized marble hydroxyapatite (MA-Hap LR) powder was further formed into 2-3mm pellets by extrusion spheronization technique using a polyvinyl alcohol binder. Continuous column defluoridation studies were conducted to obtain optimized column parameters such as input fluoride concentration, column inflow rates, optimum pellet size, and adsorbent bed parameters to obtain maximum fluoride adsorption capacity. The best breakthrough column performance was a maximum adsorption capacity of 1.21mg/g, treating 10mg/L fluoride concentration. The optimized column flow rate was at 1 LPH using an adsorbent bed height of 25cm, which processed 28.5-bed volumes at an adsorbent exhaustion rate of 7.4g/L. The column breakthrough performance data were fit into various kinetic models (Thomas model and Yoon-Nelson model) to describe adsorption kinetics and obtain correlation coefficients. Thomas's model fitted well with a high correlation coefficient value. Modelling studies indicate MA-Hap as a promising adsorbent for drinking water treatment, and optimum column design parameters were identified for scale-up for real applications.

Formulation and Evaluation of Castor Oil Containing Self-emulsifying Pellets by Using Design of Experiment

Abstract: Background/Objectives: The objective of the study was to examine the feasibility of extrusion/ spheronization techniques for formulation of castor oil loaded self-emulsifying pellets. The study was also aimed at optimization of the self-emulsifying pellet system with design of experiments. Materials and Methods: Various surfactants and co-surfactants were tested for their ability to emulsify castor oil. The proportion of components (castor oil, surfactant and co-surfactant) in self-emulsifying pellets was optimized using a D-optimal mixture design. During optimization, the effect of composition of oil(X1), surfactant(X2) and cosurfactant(X3) blend on responses like dispersion time (Y1), resultant globule size (Y2) and polydispersity index (Y3) was studied. The developed self-emulsifying mixture was further loaded on pellet formulation using extrusion spheronization technique. Results: The application of D-optimal mixture design resulted in 16 batches, out of which the optimized batch consists of castor oil (30.92%), Cremophore EL (58.56%) and PEG 400(10.51%) having dispersion time of 53 sec, globule size of 242 nm and polydispersity index of 0.243 with desirability value of 1. All the formulation components affected the performance of pellets significantly. Free flowing pellets were obtained with 30% of oil loading. Conclusion: The self-emulsifying pellets of castor oil were successfully optimized with mixture design. The developed system containing castor oil can be used for orally for conditions like arthritis or can also serve as a carrier system for any drug or herbal active. Keywords: Solid self-emulsifying drug delivery system, Castor oil, Self-emulsifying pellets, Extrusion spheronization, Dispersion time.

Formulation Development and Invitro Evaluation of Gliclazide Pellets using Superdisintegrants by Extrusion Spheronization Technique

Introduction: Gliclazide is a sulfonylurea derivative used for the treatment of type 2 Diabetes, it is an anti-diabetic drug it is marketed under the brand name Diamicron. It is taken orally and used when dietary changes, lack of exercise, and weight loss are not sufficient. &#x0D; Aim: The principal objective of this work was to develop, formulate and evaluate the pellet formulations prepared with the incorporation of different super disintegrants in different ratios and in different combinations. In this research work, the drug gliclazide was chosen as a model drug and it was formulated into fast-dissolving pellets, which can be compressed into pelltabs and can also be filled into capsules. &#x0D; Methods: Pellets were prepared by extrusion and Spheronization containing microcrystalline cellulose (MCC) and using gliclazide as a model drug with different super disintegrants namely croscarmellose sodium, crospovidone and sodium starch glycolate in different ratios, and in different combinations. Thus, in the present study, gliclazide pellets were developed using Extrusion-Spheronization for immediate drug delivery. The pellets were evaluated for percentage drug content, flow properties, friability, size analysis, shape analysis, disintegration test, and dissolution studies. Preformulation studies were then performed using solubility studies, partition co-efficient studies, infrared spectroscopy, and drug-excipients compatibility studies between the drug and selected excipients (croscarmellose sodium, crospovidone, and sodium starch glycolate) investigated.&#x0D; Results: Formulations containing MCC, super disintegrants, and drugs in different ratios of 60/0/40, 55/5/40, and 50/10/40 w/w of croscarmellose sodium, crospovidone, and sodium starch glycolate were found to show faster release of the drug for 9 hours. Croscarmellose sodium releases the drug as it disintegrates the &#x0D; &#x0D; pellets. Sodium starch glycolate releases the drug by inducing swelling in the pellet &#x0D; matrix. Unlike the other two super disintegrants, there was no apparent change in the swelling capability of the pellets of polymer crospovidone (Polyplasdone XL10) in water. The percentage increase in diameter for Ac-Di-Sol (croscarmellose sodium), Primojel (sodium starch glycolate), and Polyplasdone XL10 were 104%, 251%, and 29% in water.&#x0D; Conclusions: Various types of super disintegrants can be investigated for their suitability in formulating pellets. In vivo drug release rate, and bioavailability studies on animals and humans may be carried out to assess the superiority of the pellets over the tablet dosage form.

Enhanced CO2 Capture Durability and Mechanical Properties Using Cellulose-Templated CaO-Based Pellets with Steam Injection during Calcination

Cellulose-templated CaO-based pellets were prepared via an extrusion–spheronization method. However, the CO2 capture capacity of the modified sorbents still deteriorated rapidly after multiple cycles, and the mechanical properties were also reduced. Steam injection during calcination was conducted to enhance the CO2 capture performance of the sorbents. The modified pellets with 10 vol % steam injection present a faster carbonation rate compared to sorbents calcined under higher steam concentrations. A CO2 uptake of 0.32 g/g was obtained after 20 cycles, 133 and 60% higher than the raw sorbent and modified sorbent without steam reactivation. Moreover, the simultaneous thermal and atmosphere-induced sintering resulted in a nearly 4 times enhancement of the mechanical strength of the sorbents from 3.9 to 14.7 N. Under the harsh environment (calcined at 950 °C), the presence of steam further aggravated the sintering of the sorbent, resulting in a dramatic decrease in CO2 uptake.

Preparation and Characterization of a Novel Multiparticulate Dosage Form Carrying Budesonide-Loaded Chitosan Nanoparticles to Enhance the Efficiency of Pellets in the Colon.

An attempt was made to conquer the limitation of orally administered nanoparticles for the delivery of budesonide to the colon. The ionic gelation technique was used to load budesonide on chitosan nanoparticles. The nanoparticles were investigated in terms of size, zeta potential, encapsulation efficiency, shape and drug release. Then, nanoparticles were pelletized using the extrusion-spheronization method and were investigated for their size, mechanical properties, and drug release. Pellets were subsequently coated with a polymeric solution composed of two enteric (eudragit L and S) and time-dependent polymers (eudragit RS) for colon-specific delivery. All formulations were examined for their anti-inflammatory effect in rats with induced colitis and the relapse of the colitis after discontinuation of treatment was also followed. The size of nanoparticles ranged between 288 ± 7.5 and 566 ± 7.7 nm and zeta potential verified their positive charged surface. The drug release from nanoparticles showed an initial burst release followed by a continuous release. Pelletized nanoparticles showed proper mechanical properties and faster drug release in acidic pH compared with alkaline pH. It was interesting to note that pelletized budesonide nanoparticles released the drug throughout the GIT in a sustained fashion, and had long-lasting anti-inflammatory effects while rapid relapse was observed for those treated with conventional budesonide pellets. It seems that there is a synergistic effect of nanoformulation of budesonide and the encapsulation of pelletized nanoparticles in a proper coating system for colon delivery that could result in a significant and long-lasting anti-inflammatory effect.

Formulation Development and Optimization of Multiparticulate System by Extrusion Spheronization Method

Aim: This study aimed at formulating and optimizing the multiparticulate system of Rifaximin by adopting 32 factorial designs with independent variables X1 and X2 as concentrations of two excipients.&#x0D; Methodology: The pellets were prepared by the Extrusion Spheronization method and evaluated for percentage yield, flow property, percentage drug content, friability, and in-vitro percentage cumulative drug release.&#x0D; Results: The optimized batch (OR7) displayed excellent flow properties, 0.15±0.03% friability, and 97.85±0.22% drug content with a cumulative drug release of 93.24±0.95%.&#x0D; Conclusion: The results confirm the usefulness of factorial design to identify the effect of variables on pellet characteristics. The optimized batch can further be coated with different polymers to obtain targeted drug delivery.&#x0D; Place of Study: Department of Pharmaceutics, M. C. E. Society’s Allana College of Pharmacy, Pune.

FORMULATION OF MESALAMINE-LOADED RECTAL MUCOADHESIVE PELLETS FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE USING 32FULL FACTORIAL DESIGN

Objective: The objective of the present work was to optimize a rectal suppository containing mucoadhesive pellets of Mesalamine to achieve local yet sustained release of Mesalamine for once-a-day administration for the therapy of Inflammatory Bowel Disease. Methods: Thus, the present work involves forming mucoadhesive pellets of mesalamine by extrusion spheronization, which were then loaded into a suppository to be administered rectally. The pellets were evaluated for mucoadhesion strength, swelling potential, morphology, particle size, drug release, drug loading and retention time. Results: The optimized batch of pellets using Eudragit RLPO as the release retardant, carrageenan as a mucoadhesive polymer and other excipients had a mucoadhesion strength of 0.143 N, a swelling index of 50.50 %, and 44 % and 75 % drug was released from them at the end of 6 and 15 h respectively. The pellets-loaded cocoa butter suppositories had a melting range of 35–37 °C, disintegrated within 8–9 min and had a hardness of 4–5 kg/cm3. A comparison of the in vitro drug release profile from the mucoadhesive pellets and the mucoadhesive pellets-loaded suppositories showed a closeness in the % cumulative drug release indicating that cocoa butter did not interfere in the release of the drug from the pellets. Conclusion: Mucoadhesive Pellets were successfully developed by extrusion spheronizer technique and incorporated into suppositories. In vitro study revealed a release profile that warranted a once-a-day regimen leading to a reduction in the requirement of the drug and hence the side effects.

Formulation Development of Sustained Release Matrix Pellets Compressed into Unit Dosage Form

&gt;Any drug delivery system’s main objective is to consistently deliver the desired drug concentration in the blood or tissues, which is therapeutically beneficial and non-toxic. The spherical, free-flowing granules known as pellets increase bioavailability, lower the risk of dose dumping and local gastrointestinal discomfort, regulate drug release, and boost absorption of the medicine. A second-generation sulfonylurea called gliclazide is used to treat non-insulin-dependent diabetic mellitus (NIDDM). This study’s objectives were to construct a flexible dosage form with controlled release and look into how process parameters affected the procedure. To find the batch of pellets that provided a sustained release pattern for the drug gliclazide, several batches of pellets manufactured using the extrusion spheronization process and the design of experiment (DoE) approach were used. Due to their roundness, the pellets had excellent flow characteristics, which affected the dosage production rate. They also had small particles that could be easily dispersed and helped prevent dosing. The release rate of the pellets was 99.3% after 12 hours. With superior medication release control, the study completes the development of sustained-release pellets, minimizing issues with the conventional tablet administration form.