Formulation Factors Research Articles

Assessment of Risk Factors for Formulation of Kidney Stone among Adult Males

Assessment of Risk Factors for Formulation of Kidney Stone among Adult Males

Assessment of nano lipid carrier loaded transdermal patch of rizatriptan benzoate.

Migraine is a neurological disorder and is accompanied by different painful episodes. Hence the maintenance of a steady-state concentration of drug can be beneficial for the patients suffering with migraine. The present investigation focuses on the development of nano lipid carriers (NLCs) loaded transdermal patch of rizatriptan benzoate to sustain the effect of the drug for the enhancement of therapeutic effects. Stearic acid and peanut oil were used to make the NLCs. A central composite design was employed to observe the effect of formulation factors like solid lipid ratio, phase volume ratio, and concentration of surfactants on the formation of nanoparticles. The effects were evaluated for the responses like particle size and entrapment of the drug in the nanocarriers. The optimized formulation was subjected to compatibility, thermal, surface characteristics, and surface morphology studies. The optimized formulation was dispersed in HPMC 15CPS and PVP K30 polymer matrix and the transdermal patch was evaluated for its mechanical properties, drug release study, and skin irritation study. The experimental design was suitable to produce nanosized stable lipid carriers of the drug with high drug entrapment. The drug and excipients were found to be compatible. The thermal and surface characteristics study proved the high loading of drug in the nanoparticles. The surface morphology study showed the formation of irregular-shaped NLCs. The transdermal patch had good mechanical properties. The ex vivo study of the formulated patch showed a sustained release of the drug over 24h. No skin irritation was reported from the transdermal patch. Therefore, it can be concluded that the nanoparticles loaded transdermal patch of rizatriptan benzoate can be promising in controlling the divergent phases of migraine.

Convective Solvent Transport Pathways for Absorption of Drugs from Topical Formulation.

Physicochemical and formulation factors influencing penetration of drugs from topical products into the skin and mechanisms of drug permeation are well investigated and reported in the literature. However, mechanisms of drug absorption during short-term exposure have not been given sufficient importance. In this project, the extent of absorption of drug molecules into the skin from aqueous and ethanolic solutions following a 5-min application period was investigated. The experiments demonstrated measurable magnitude of absorption into the skin for all the molecules tested despite the duration of exposure being only few minutes. Among the two solvents used, absorption was greater from aqueous than ethanolic solution. The results suggest that an alternative penetration pathway, herein referred to as the convective transport pathway, is likely responsible for the rapid, significant uptake of drug molecules during initial few minutes of exposure. Additionally, absorption through the convective transport pathways is a function of the physicochemical nature of the formulation vehicle rather than the API.

Application of Emax model to assess the potency of topical corticosteroid products.

The objective of this study was to compare the potencies of two topical corticosteroid products (TCPs) using the Emax model to fit the skin blanching responses obtained from the US FDA's vasoconstrictor assay (VCA) and to illustrate the influence of formulation on potency. The potencies of two marketed TCPs, Dermovate® cream containing clobetasol propionate (CP) and Elocon® cream containing mometasone furoate (MF), were assessed using healthy human subjects. In order to investigate the influence of formulation and associated vehicle properties, the creams were compared with their respective topical corticosteroids (TCs) from a previously published study wherein the inherent potencies of those TCs were assessed using a validated VCA method. Whereas the inherent potency of MF (Emax = -94.45 ± 0.21) was found to be greater than CP (Emax = -58.80 ± 15.65), when formulated as creams, the TCP containing CP had a higher potency (Emax = -86.15 ± 0.17) than that containing MF (Emax = -42.61 ± 26.04). This reversal of potency may be attributed to the effect of formulation factors. The comparison of the potencies of TCPs with inherent potencies of their corresponding TCs confirmed the influence of formulation parameters on the potency of those products.

Development and characterization of gastro-floating sustained-release capsule with improved bioavailability of levodopa.

In this study, a new gastro-floating sustained-release capsule (GFC) with levodopa (LD) and benserazide hydrochloride (BH) was successfully developed. GFCs were prepared by filling the LD and BH granules into hard capsules and coated with cellulose acetate (CA) solution as a controlled-release layer. The effects of formulation factors on the release of GFCs were conducted. The AUC0~24 (µgh/mL) of LD were 69.31 ± 3.61 (μgh/mL) and 28.87 ± 2.58 (μgh/mL) and the Cmax were 7.84 ± 0.34 (μg/mL) and 9.21 ± 1.04 (μg/mL) in the GFCs and commercial tablets respectively. The relative bioavailability of LD was 267.55 ± 34.54%. Compared with commercial tablets, the pharmacokinetic study indicated that the developed GFCs provided a better sustained-release effect and higher bioavailability than commercial tablets.

Review of nanosuspension formulation and process analysis in wet media milling using microhydrodynamic model and emerging characterization methods

Wet media milling is a popular technology used to prepare nanosuspensions. However, the theories and methods to guide the research on the formulation and process affecting wet media milling remain limited. The research on wet media milling follows a “black box” approach to a certain extent. This review focuses on exploring the formulation and process parameters factors in wet media milling. The formulation factors include the concentration, hydrophilicity/hydrophobicity, and structure of the drug and stabilizer, whereas the milling process parameters include the milling speed, milling time, and material, size, and filling volume of milling beads. Contrary to other reviews, this review attempts to quantify and visualize these factors by combining a microhydrodynamic model with emerging characterization methods to provide a scientific basis for the selection of nanosuspension formulations and process parameters, as opposed to the conventional trial-and-error approach.

DEVELOPMENT OF SYSTEMIC MEASURES TO IMPROVE THE QUALITY OF THE EDUCATIONAL PROCESS AT THE NATIONAL TRANSPORT UNIVERSITY

The article is devoted to the consideration of an actual issue - the development of systemic measures to improve the quality of the educational process at the National Transport University. R. Mitchell's model was applied to classify the stakeholders of the higher education institution depending on their interests. The stages of creating coalitions of stakeholders are proposed, which include drawing up a list of stakeholders; grouping of stakeholders according to their interests, position, degree of influence and priority value; determination of stakeholders' influence factors for strategy formulation and decision-making; assessment of factors and integration of stakeholders' interests; development of improvement measures taking into account the interests of stakeholders. The four main stakeholder coalitions of the National Transport University were identified, a map of their interests was developed, and the results of the questionnaire regarding the quality of the educational process for the 2021-2022 academic year were analyzed. A list of measures for the development of the system for ensuring the quality of the educational process in the 2022-2023 academic year has been developed, including: gradual introduction of elements of education in the dual form of education; deepening cooperation with employers, in particular, involving employers in the organization of the educational process according to the educational programs of the university; systematic work on the motivation of teachers to improve their teaching skills and publish articles in international scientometric databases, participate in international projects, improve their knowledge of foreign languages; intensification of the use of software products in the educational process; expanding the functionality of distance learning platforms and services used by the university; strengthening of internal monitoring of educational programs; use of a flexible mode of online classes (synchronous / asynchronous mode). It is proposed to develop the research data in the development of a strategic model of the university's development.

Design and Fabrication of Gallic Acid Loaded Chitosan Nanoformulation

Background: Gallic acid is a natural phenolic compound found in several fruits and me-dicinal plants. It is reported to have several health-promoting effects, including antioxidant, anti-inflammatory, antidiabetic, and antineoplastic properties in gastrointestinal, neuropsychological, metabolic, and cardiovascular disorders. Aims: The aim of the present work was to study the influence of formulation factors on the physi-cochemical properties of gallic acid-loaded chitosan nanoparticles in order to optimize the formula-tion. Methods: Active chitosan nanoparticles could be used to support the modification of gallic acid delivery. The nanoparticles were prepared by the emulsification-solvent evaporation method using sonication. A 3-factor, 2-level BBD (Box-Behnken Design) was applied for exploring and opti-mizing the main effects, quadratic effects, as well as interaction effects of the ingredients of the formulation on the performance of the nanoparticles. The responses like particle size, poly-dispersity index, zeta potential, and encapsulation efficiency were also determined. Results: The concentration of gallic acid nanoparticles seems to be the most critical element affect-ing their properties. The concentration of chitosan was increased, which resulted in an increase in particle size. The optimised drug-loaded nanoparticles have a zeta potential of -5.2 mV due to their largely negative surface charge. Although the measured zeta potential was low, the nanoparticle dispersion remained stable, and no significant change in the shape or particle size of the gallic acid-loaded chitosan nanoparticles was seen after two weeks at 4°C. The gallic acid-loaded nanoparticles have a particle size of 230 nm. Gallic acid reduced the particle size after it was added. One probable explanation for this is that the loaded medicine increased the cohesive force of the hydrophobic con-tact, resulting in the size reduction. A formulation was optimised based on the acquired results, and the experimental values were comparable to the expected values. FTIR examination revealed that gallic acid-loaded chitosan nanoparticles displayed both hydrogen bond and ionic interactions, al-lowing for active agent encapsulation and augmentation. Conclusions: The overall results indicated that by decreasing the chitosan concentration, drug en-trapment efficiency increased and gallic acid concentration was the main factor influencing particle size, while entrapment efficiency was predominantly affected by the chitosan concentration.

Optimization of the Preformulation and Formulation Parameters in the Development of New Extended-Release Tablets Containing Felodipine

Herein, new extended-release tablets containing felodipine were developed. For the orally administered formulations, optimization of the preformulation and formulation parameters was performed to assess the performance of the dosage form. Initially, the morphological and physical characterization of two forms of felodipine (microcrystalline and macrocrystalline) using Fourier transform infrared spectroscopy, differential scanning calorimetry and optical microscopy was performed. The pharmaco-technical properties of the two felodipine forms were also determined. Subsequently, formulation studies for felodipine extended-release tablets were performed. Mathematical modelling of release kinetics of felodipine from developed formulations using a power law model was also performed. Based on the influence of formulation factors on the in vitro availability of felodipine in experimental tablets, a new extended-release tablet formulation was established.

Development and Characterizations of Pullulan and Maltodextrin-Based Oral Fast-Dissolving Films Employing a Box-Behnken Experimental Design.

Migraine is a neurological disorder characterized by severe headaches, visual aversions, auditory, and olfactory disorders, accompanied by nausea and vomiting. Zolmitriptan (ZMT®) is a potent 5HT1B/1D serotonin receptor agonist frequently used for the treatment of migraine. It has erratic absorption from the gastrointestinal tract (GIT), but its oral bioavailability is low (40–45%) due to the hepatic metabolism. This makes it an ideal candidate for oral fast dissolving formulations. Hence, the current study was undertaken to design and develop oral fast-dissolving films (OFDFs) containing ZMT for migraine treatment. The OFDFs were formulated by the solvent casting method (SCM) using Pullulan (PU) and maltodextrin (MDX) as film-forming agents and propylene glycol (PG) as a plasticizer. The strategy was designed using Box–Behnken experimental design considering the proportion of PU:MDX and percentage of PG as independent variables. The effectiveness of the OFDF’s was measured based on the following responses: drug release at five min, disintegration time (D-time), and tensile strength (TS). The influence of formulation factors, including percent elongation (%E), thickness, water content, moisture absorption, and folding endurance on ZMT-OFDFs, were also studied. The results showed a successful fabrication of stable ZMT-OFDFs, with surface uniformity and amorphous shape of ZMT in fabricated films. The optimized formulation showed a remarkable rapid dissolution, over 90% within the first 5 min, a fast D-time of 18 s, and excellent mechanical characteristics. Improved maximum plasma concentration (C max) and area under the curve (AUC 0–t) in animals (rats) treated with ZMT-OFDFs compared to those treated with an intra-gastric (i-g) suspension of ZMT were also observed. Copolymer OFDFs with ZMT is an exciting proposition with great potential for the treatment of migraine headache. This study offers a promising strategy for developing ZMT-OFDFs using SCM. ZMT-OFDFs showed remarkable rapid dissolution and fast D-time, which might endeavor ZMT-OFDFs as an auspicious alternative approach to improve patient compliance and shorten the onset time of ZMT in migraine treatment.

Understanding Formulation and Temperature Effects on Dermal Transport Kinetics by IVPT and Multiphysics Simulation

It is often unclear how complex topical product formulation factors influence the transport kinetics through skin tissue layers, because of multiple confounding attributes. Environmental factors such as temperature effect are also poorly understood. In vitro permeation testing (IVPT) is frequently used to evaluate drug absorption across skin, but the flux results from these studies are from a combination of mechanistic processes. Two different commercially available formulations of oxybenzone-containing sunscreen cream and continuous spray were evaluated by IVPT in human skin. Temperature influence between typical skin surface temperature (32°C) and an elevated 37°C was also assessed. Furthermore, a multiphysics-based simulation model was developed and utilized to compute the flux of modeled formulations. Drug transport kinetics differed significantly between the two drug products. Flux was greatly influenced by the environmental temperature. The multiphysical simulation results could reproduce the experimental observations. The computation further indicated that the drug diffusion coefficient plays a dominant role in drug transport kinetics, influenced by the water content which is also affected by temperature. The in vitro testing and bottom-up simulation shed insight into the mechanism of dermal absorption kinetics from dissimilar topical products.

Development and optimization of ofloxacin as solid lipid nanoparticles for enhancement of its ocular activity

Ofloxacin (Ofx) is one of the most commonly available ocular antibiotic solutions. Unfortunately, it suffers from rapid tear turnover and therefore requires administration every 4 h or even every hour for serious eye infections; moreover, its solubility is pH-dependent and very low at the pH of corneal fluid (7.2–7.4), and it can form a white crystalline deposit on the cornea. Hence, the aim of this investigation was to load Ofx into solid lipid nanoparticles (SLNs) to address its limitations. SLNs were prepared using hot homogenization followed by ultrasonication techniques at a pH of 7.4. The Box-Behnken design addressed the influence of the formulation factors, namely, the effects of the percentages of Compritol, Gelucire 44/14, and stearylamine on the particle size, zeta potential, entrapment efficiency, percentage of Ofx release after 1 h, and time required to release 50% of the drug. The obtained optimal Ofx-SLN was evaluated for its transcorneal permeation, antimicrobial activity, and amount of Ofx present in the aqueous humor as compared with Ofx aqueous suspension, and commercially available Ofx eye drop. The optimum formulation exhibited a particle size of 34 nm, zeta potential of 22 mV, entrapment efficiency of 82%, Ofx release of 9% after 1 h, and time to release of 50% of the drug of 5 h. It produced a 1.5-fold and 3-fold increase in the cumulative amount permeated and cumulative percentage permeated, respectively, compared with other tested formulations. Furthermore, the optimized Ofx-SLN had a high level over the minimum inhibitory concentration in the aqueous humor of rabbits for longer periods compared with a commercial preparation. These data proved that a once-a-day dose of an Ofx-SLN dispersion would produce the required effects of prolonged transcorneal permeation, enhanced ophthalmic bioavailability, diminished need for recurrent administration.

The Trending Role of Artificial Intelligence and Its Applications in Formulation of Solid Dosage Forms: A Review

Artificial intelligence (A.I) is a technology based system involved in use of advanced tools and software’s and has achieved human level of capabilities and brought a paradigm shift in pharma industry therefore use of A.I in pharmaceutical product development has elevated over past few years. Adopting of technology can save money and time also provide good understanding between formulation and process parameters. Solid dosage forms are predominant in pharmaceutical market. It is estimated that tablets are the most come solid dosage form which contributes more than two-third of global market. Tablets are produced with many formulation factors i.e. from raw material to finished product therefore it is a great task and often complicated. Thus the use of A.I can help to obtain optimized formulations which could benefit pharmaceutical industry massively. Therefore adopting A.I–based technologies in manufacturing process of pharmaceutical product will improve the quality and safety of the product.

Formulation, optimization, and in vitro evaluation of anastrozole-loaded nanostructured lipid carriers for improved anticancer activity

The present study aims to develop and optimize anastrozole (ANZ)-nanostructured lipid carriers (ANZ-NLCs) for improved anticancer efficacy. In a nutshell, ANZ-NLCs were prepared by a 32 factorial design approach through the solvent evaporation method. In this study, key formulation factors impacting particle size, % drug encapsulation, and zeta potential were optimized in ANZ-NLCs. The physicochemical characterization and in vitro cytotoxicity, cell apoptosis, cell cycle analysis, cell uptake, and investigation of apoptotic nuclei by DAPI study was performed on MCF 7 to assess the potential of ANZ-NLCs. The optimized batch exhibited the spherical and smooth surface morphology that was confirmed by AFM and HR-TEM. In addition, the optimized batch showed 164.4 nm particle size, 62.95% entrapment efficiency, and −26.3 mV zeta potential. Elucidation of FTIR and H NMR studies revealed compatibility of ANZ with the carrier lipids and DSC and XRD confirmed amorphous ANZ-NLCs (which was the type of NLC formed). The in vitro ANZ release study revealed the significance of compritol in release modulation from ANZ-NLCs. Herein, the optimized batch demonstrated extended-release in different release media (upto 48 h), following the fickian type. In vitro anticancer efficacy was assessed by cytotoxicity, cell apoptosis, cell cycle analysis, cell uptake, and apoptotic nuclei, which confirmed the significant anticancer efficacy of ANZ-NLCs compared to free ANZ. Consequently, ANZ-NLCs made from compritol 888 ATO and capryol could be a prospective formulation exhibiting significant anticancer potential in the oral delivery of ANZ for the effective dealing of breast cancer (BC).

Influence of Formulation Factors, Process Parameters, and Selected Quality Attributes on Carvedilol Release from Roller-Compacted Hypromellose-Based Matrix Tablets.

The importance of roller compaction is recently increasing. This study evaluates the combined effects of formulation factors, process parameters, and selected quality attributes on drug release from roller-compacted hypromellose-based matrix tablets containing carvedilol as a model drug. The influence of selected factors was statistically assessed and good predictive models were developed for various time points of the release profile. The results show that the release profile is mostly affected by the particle size distribution of granules and roll speed. This indicates that the roller compaction process has a major impact on drug release, which is also formulation dependent. A higher d50 and lower d90 value of spatial filtering technique-based particle size distribution results, a lower roll speed, increased hypromellose content, using microcrystalline cellulose as a filler, and higher tablet hardness, resulted in a decrease in the drug release rate. On the other hand, the effect of the roll pressure, size of screen apertures, and d10 values on drug release was insignificant. The significance of the factors was further explained by granule shape, their porosity, and friability evaluation, and by compressibility and compactibility studies of compression mixtures. Additionally, the spatial filtering technique demonstrated to be a promising tool in controlling the roller compaction process.

Design of polymeric nanoparticles for oral delivery of capreomycin peptide using double emulsion technique: Impact of stress conditions

Peptides are short polymers of amino acids that are unstable at drastic conditions including highly acidic or highly alkaline media, high temperature and high shear forces. Polymeric nanoparticles as carrier for peptides are the most desirable formulation in pharmaceutical field than other colloidal systems because of their stability in biological environment. Two different biodegradable polymers were chosen to formulate nanoparticles as carriers for capreomycin sulfate (CMS) peptide. Chitosan was selected as a water soluble polymer, while, poly(lactic-co-glycolic) acid (PLGA) polymer is soluble in organic solvents. Double emulsion solvent evaporation technique was used in the formulation of the nanoparticles. This method required applying of thermal, mechanical and chemical stresses that could have impact on peptide degradation that should be considered in the design of nanoparticles. Many formulation factors for polymeric nanoparticles optimization were tested including: probe sonication intensity and time, homogenization speed, pH of dispersion media, drug:polymer ratios, type and concentration of crosslinking agents and concentration of the stabilizer. Controlling these factors with monitoring of peptide degradation allowed to optimize polymeric nanoparticles having the smallest possible particle sizes (343.7–1656.5 nm) with the highest entrapment efficiencies (17.30–62.30%). The produced polymeric nanoparticles were tested for in vitro drug release in phosphate buffer pH 6.8. Different CMS release profiles were observed (15.52–72.44%) where PLGA NPs showed significant slower release compared with that of chitosan NPs.

Formulation of oxybutynin chloride microparticle-loaded suppositories: in vitro characterization and in vivo pharmacokinetic study

BackgroundOxybutynin chloride (OXC) is used to treat overactive urinary bladder. OXC is metabolized in the liver to N-desethyloxybutynin, which is mainly responsible for the anticholinergic side effects of OXC. Conventional oxybutynin suppositories formulated earlier have shown most common side effects, such as dry mouth, constipation and serious anticholinergic reaction. Hence the present research work deals with the formulation and characterization of OXC microparticle-loaded mucoadhesive suppositories which may remain adhered in the lower rectum and avoid first pass metabolism. The emulsification–ionic gelation method is employed to prepare OXC microparticles. Two formulation factors at three levels, i.e. polymer concentration and stirring speed, were selected. Sodium alginate (concentration 1–2%) and 1% w/v Carbopol 971P were used to prepare OXC microparticles. OXC microparticles were evaluated for various parameters such as production yield, entrapment efficiency, mucoadhesive strength, shape, size, zeta potential, Fourier Transform Infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, in vitro dissolution studies and stability studies. Suppositories loaded with OXC microparticles were prepared by the fusion method using Poloxamer 188 and propylene glycol and evaluated for various parameters like weight variation, disintegration time, in vitro dissolution study, stability study and pharmacokinetic study.ResultsResults of in vitro characterization revealed that optimized batch of OXC loaded microparticles exhibited production yield 94.024% entrapment efficiency 95.378% and mucoadhesion strength 95.544%, particle size range 764.04–894.13 µm, zeta potential − 14.5 mV, with 0.946 desirability. Consequences of DSC and XRPD evaluation shown that drug was effectively entrapped inside the microparticles. In vitro release studies revealed improvement in drug dissolution as a consequence of its entrapment into microparticles. SEM results showed that micelles were sphere-shaped. On rectal administration of OXC microparticles loaded suppository in male Sprague–Dawley Rats, the relative bioavailability was found 173.72%.ConclusionIn vivo study elicits rapid increase in absorption of drug from microparticles loaded suppository when compared with the oral formulation and drug loaded suppository in rats. OXC microparticles loaded suppository is novel and promising drug delivery system for rectal administration and may avoid anticholinergic side effects of hepatic metabolite, N-desethyloxybutynin. These rectal drug delivery systems will be advantageous for efficient absorption of drugs and to avoid first pass metabolism.

Exploration of the cardinal formulation parameters influencing the encapsulation and physicochemical properties of co-loaded anticancer dual drug nanoliposomes

Rationale-based modulation of physico-chemical properties is critical towards design of optimal liposomal formulations having desired pharmacokinetic and pharmacodynamic profiles. The aim of the study was evaluation of critical formulation factors which may influence the encapsulation efficiency, hydrodynamic diameter, electrokinetic potential, internal morphology and drug release profiles of nanoliposomes. Doxorubicin and Vincristine were actively co-loaded in preformed PEGylated liposomes prepared using ethanolic injection. The variation of independent factors (transmembrane gradient, lipid-molar ratio, drug loading temperature, phosphatidylcholine chain length, sequence of drug addition, drug loading pH, external medium) on dependent variables were evaluated using array of univariate analysis with key determinants further analysed using multivariate studies. Univariate study results showed that concentration of ammonium sulphate, drug loading pH and lipid-molar ratio had significant effect on dependent variables. Nanoliposomes prepared in multivariate studies exhibited high encapsulation efficiency (>95%), particle size (Z-average: 106.55 ± 6.63 nm) and surface charge of −5.55 ± 2.77 mV. The optimized nanoliposomes exhibited characteristic coffee-bean shaped morphology showing doxorubicin nanoprecipitation and electron dense vincristine presence in internal aqueous phase that exhibited controlled in-vitro release of both drugs unaffected by presence of each other. Further, an attempt was made to correlate these results to the chemical structure and physicochemical properties of the drugs.

Consensus reaching for prospect cross-efficiency in data envelopment analysis with minimum adjustments

The expected utility theory and the arithmetic average method have been widely adopted for the cross-efficiency strategy formulation and cross-efficiencies aggregation. However, traditional cross-efficiency methods often fail to consider the decision maker’s (DM’s) risk attitude and neglect the consensus among decision-making units (DMUs) in the cross-evaluation process. Thereby, this paper utilizes the prospect cross-efficiency (PCE) model to describe the DM’s subjective preference in the evaluation process and a consensus framework to manage the consensus among DMUs in the aggregation process. First, the PCE model is utilized to derive the cross-efficiency matrix, and it can reflect DMs’ psychological factors in the strategy formulation of cross-efficiency. Then, a two-stage consensus optimization framework (TSCOF) with minimum adjustments is presented to improve the consensus degree (CD) among the DMUs in the cross-evaluation process. The TSCOF generates a sequential optimization strategy that minimizes the adjustment distance and the number of modifications sequentially. Next, we develop an interactive consensus reaching process (CRP) for PCE problems based on the consensus rule. The CRP does well in helping improve the CD among DMUs. Finally, an illustrative example related to the performance of the S&T activities of 10 universities is offered to elaborate on the feasibility and effectiveness of our approach.

IMPLEMENTATION OF FACTORIAL DESIGN TO OPTIMIZE THE FORMULATION METHOD OF EZETIMIBE POLYMERIC NANOPARTICLE BY HOMOGENIZATION CUM ULTRA-SONICATION METHOD

Objective: The objective of this study is to use a 23 factorial design to optimize the formulation factors of Ezetimibe polymeric nanoparticle. Methods: By varying formulation variables such as polymer concentration (hydroxyl propyl methyl cellulose composition) and process variables such as homogenization time (min) and ultra-sonication time, the formulation of polymeric nanoparticles was designed using a 23 factorial design and prepared using the homogenization cum ultra-sonication method (min). Particle size (nm), zeta potential (mV), polydispersity index, entrapment efficiency (%), drug content, in vitro drug release, in vitro release kinetic studies, and stability studies were used to analyse and optimize polymeric nanoparticles according to ICH criteria. Results: R7 formulation showed predicted and desired less particle size 87.0±3.64 nm; maximum zeta potential-33.4±2.32 mV; desired polydispersity index 0.488±0.20; maximum entrapment efficiency of 96.45±2.42 % and controlled dissolution release pattern of about 90.42±3.56% in 24h. Conclusion: The polymeric nanoparticle was formulated and optimized by the parameters like Particle Size (PS in nm), Polydispersity Index (PI), Zeta potential (Zp in mV), % Entrapment Efficiency and in vitro drug release for 24 h were evaluated. These parameters showed significant changes while formulating polymeric nanoparticles along with various formulation and process variables. From the release pattern data it was observed that PNs show a significant improvement of dissolution character of Ezetamibe. According to the findings, PNs have a controlled drug release pattern and can be used as a suitable drug delivery carrier for low solubility and poorly bioavailable drugs like Ezetamibe to improve its dissolution.