Nano Spray Dryer Research Articles

Inhalable resveratrol microparticles produced by vibrational atomization spray drying for treating pulmonary arterial hypertension

The rare disorder pulmonary arterial hypertension is characterized by elevated pulmonary arterial pressure and right heart failure. Currently, the treatments have improved, but a cure has not yet been discovered. In this study, we developed a new formulation using an innovative controlled delivery system for resveratrol: s dry powder inhaler form designed for pulmonary administration. The particles were composed of resveratrol, as the therapeutic agent; poly(ε-caprolactone), for structuring the controlled-release matrix; sodium deoxycholate, to prevent agglomeration; and trehalose, as drying adjuvant, respectively. The particles were obtained using the piezoelectric atomization technique with a Nano Spray Dryer B-90®. The fine particle fraction was approximately 50% and the theoretical aerodynamic diameter was 2.32 μm. The process afforded excellent yields (approximately 80%) with low powder moisture (less than 2.0%). Due to the low density and the increased flowability of the powder, the spherical shape of the particles and an irregular surface, the microparticles possessed aerodynamic properties suitable for drug deposition on the bronchial and alveolar regions of the lungs. The aerodynamic properties and in vitro sustained release profiles showed a great potential for the inhaled administration of drugs such as resveratrol suitable for the treatment of pulmonary arterial hypertension.

Effect of particle size reduction and crystalline form on dissolution behaviour of nimesulide

The objective of this study was to develop and examine innovative and very simple and easily scalable techniques able to improve solubility and/or dissolution rate and thus oral bioavailability of nimesulide. Three different nimesulide batches were obtained by three different laboratory-scale methods: Method A (Batch A) used crystallization by solvent evaporation in a nanospray dryer, Method B (Batches G and GLN) involved cryo-milling, and Method C (Batch Neu) dispersed nimesulide in Neusilin® UFL2. All the nimesulide batches were fully characterized for chemical stability, thermal behaviour, physicochemical and micromeritics properties, and intrinsic dissolution and particle dissolution rates. Batch A not only showed a good reduction in particle size but also exhibited a reduced degree of crystallinity by both differential scanning calorimetry and X-ray powder diffractometry, which could explain the increase in intrinsic dissolution rate (IDR) and particle dissolution. Batch GLN showed an acceptable increase in IDR, probably caused by a slight decrease in the degree of crystallinity, and good improvement in dissolution rate due to a certain decrease in particle size. Batches G and native crystals exhibited very close IDRs, while G showed somewhat higher particle dissolution, probably attributed to the particle size reduction. The dispersion of nimesulide in Neusilin UFL2 in a 1:6 drug–polymer ratio made it possible to recover anamorphous powder, as proven by thermal analysis and X-ray powder diffractometry, characterized by pronounced particle size reduction to nanometric dimensions. Both amorphous character and nanometric dimensions could account for the fastest particle dissolution during the first 10 min of the experiment. The stability study conducted according to the International Conference on Harmonization (ICH) confirmed the good chemical and physicochemical stability of all the batches.

Nano spray-dried sodium chloride and its effects on the microbiological and sensory characteristics of surface-salted cheese crackers

Reducing particle size of salt to approximately 1.5 µm would increase its surface area, leading to increased dissolution rate in saliva and more efficient transfer of ions to taste buds, and hence, perhaps, a saltier perception of foods. This has a potential for reducing the salt level in surface-salted foods. Our objective was to develop a salt using a nano spray-drying method, to use the developed nano spray-dried salt in surface-salted cheese cracker manufacture, and to evaluate the microbiological and sensory characteristics of cheese crackers. Sodium chloride solution (3% wt/wt) was sprayed through a nano spray dryer. Particle sizes were determined by dynamic light scattering, and particle shapes were observed by scanning electron microscopy. Approximately 80% of the salt particles produced by the nano spray dryer, when drying a 3% (wt/wt) salt solution, were between 500 and 1,900 nm. Cheese cracker treatments consisted of 3 different salt sizes: regular salt with an average particle size of 1,500 µm; a commercially available Microsized 95 Extra Fine Salt (Cargill Salt, Minneapolis, MN) with an average particle size of 15 µm; and nano spray-dried salt with an average particle size of 1.5 µm, manufactured in our laboratory and 3 different salt concentrations (1, 1.5, and 2% wt/wt). A balanced incomplete block design was used to conduct consumer analysis of cheese crackers with nano spray-dried salt (1, 1.5, and 2%), Microsized salt (1, 1.5, and 2%) and regular 2% (control, as used by industry) using 476 participants at 1wk and 4mo. At 4mo, nano spray-dried salt treatments (1, 1.5, and 2%) had significantly higher preferred saltiness scores than the control (regular 2%). Also, at 4mo, nano spray-dried salt (1.5 and 2%) had significantly more just-about-right saltiness scores than control (regular 2%). Consumers’ purchase intent increased by 25% for the nano spray-dried salt at 1.5% after they were notified about the 25% reduction in sodium content of the cheese cracker. We detected significantly lower yeast counts for nano spray-dried salt treatments (1, 1.5, and 2%) at 4mo compared with control (regular) salt (1, 1.5 and 2%). We detected no mold growth in any of the treatments at any time. At 4mo, we found no significant differences in sensory color, aroma, crunchiness, overall liking, or acceptability scores of cheese crackers using 1.5 and 1% nano spray-dried salt compared with control. Therefore, 25 to 50% less salt would be suitable for cheese crackers if the particle size of regular salt was reduced 3 log to form nano spray-dried salt. A 3-log reduction in sodium chloride particle size from regular salt to nano spray-dried salt increased saltiness, but a 1-log reduction in salt size from Microsized salt to nano spray-dried salt did not increase saltiness of surface-salted cheese crackers. The use of salt with reduced particle size by nano spray drying is recommended for use in surface-salted cheese crackers to reduce sodium intake.

Optimization of the Büchi B-90 spray drying process using central composite design for preparation of solid dispersions

A central composite design approach was applied to study the effect of polymer concentration, inlet temperature and air flow rate on the spray drying process of the Büchi B-90 nano spray dryer (B-90). Hypromellose acetate succinate-LF was used for the Design of Experiment (DoE) study. Statistically significant models to predict the yield, spray rate, and drying efficiency were generated from the study. The spray drying conditions were optimized according to the models to maximize the yield and efficiency of the process. The models were further validated using a poorly water-soluble investigational compound (BI064) from Boehringer Ingelheim Pharmaceuticals. The polymer/drug ratio ranged from 1/1 to 3/1w/w. The spray dried formulations were amorphous determined by differential scanning calorimetry and X-ray powder diffraction. The particle size of the spray dried formulations was 2–10μm under polarized light microscopy. All the formulations were physically stable for at least 3h when suspended in an aqueous vehicle composed of 1% methyl cellulose. This study demonstrates that DoE is a useful tool to optimize the spray drying process, and the B-90 can be used to efficiently produce amorphous solid dispersions with a limited quantity of drug substance available during drug discovery stages.

A Design of Experiment Study of Nanoprecipitation and Nano Spray Drying as Processes to Prepare PLGA Nano- and Microparticles with Defined Sizes and Size Distributions.

Aim of this study was to explore the potential of a design of experiments approach to nanoprecipitation (NPR) and nano spray drying (NSD) as processes for preparing poly (lactic-co-glycolic acid, PLGA) nano- and microparticles. In particular, we determined the feasible size range, critical factors influencing particle size, size distribution or yield, and the robustness towards variations of the batch size. A fractional factorial design for response surface was applied to study the influence on continuous, categorical and discrete factors. NPR yielded nanoparticles (150-200nm) with narrow size distribution (PDI < 0.15). Polymer concentration was the main factor in this process, which was found to be very robust to varying the batch size (0.625-50.0ml). In contrast, NSD yielded microparticles (2-163μm). The latter process appeared, however, to be influenced by various factors and, therefore, more difficult to control and less robust towards varying the batch size (5-40ml). By a factorial design approach to NPR, we succeeded to derive an equation, which allowed the prediction of several optimal formulations with defined particle sizes and distributions. DOE can help to understand innovative manufacturing processes for nano- and microparticulate drug delivery systems, as well as to optimize these processes regarding particle size, size distribution and yield. Such understanding of these processes is instrumental for their subsequent scale up and quality control as needed for preclinical and clinical test batches.

Novel Drying Technology of Microsphere and Its Evaluation for Targeted Drug Delivery for Lungs

Carbopol microspheres of methotrexate (MxtCM), a drug used in the treatment of lung cancer, were prepared using a Buchi B-90 nano spray dryer. The surface morphology was found to be shriveled to nearly spherical, with an average size of 6.8 µm. The drug loading and percentage yield were found to be 77% ± 0.3% and 89% ± 0.4%, respectively. The in-vitro release was suggestive of the Baker and Lonsdale model, as the release pattern involved swelling and diffusion; the total methotrexate release after 12 h was 98.2% from MxtCM while, for the pure drug, it was 94.2% at 0.5 h. Liquification was witnessed during the stability studies at 37°C and at a relative humidity of 75%. This study concludes that the microsphere could be one of the most appropriate drug delivery methods for the successful delivery of methotrexate to the lungs. The pharmacokinetic (drug concentration) results following intravenous administration were 1,021 µg/g after 15 min; in comparison, in the spleen and liver, the concentration of the conventional dosage of Mxt was <401 µg/g after 10 min. We concluded that the methotrexate concentration was increased in the lungs when compared to the blood, spleen, and liver. The ingredients used in the formulation were confirmed harmless from histopathological studies. Thus, microspheres can be adopted in formulating and targeting methotrexate to the lungs.

Cross-linking of Horseradish Peroxidase Enzyme to Fine Particles Generated by Nano Spray Dryer B-90

Enzymatic methods can be effective tools for removal of phenolic compounds from wastewater by forming reactive radicals with polymerization mechanism. Comparing with conventional chemical ways, enzymes have advantages such as low cost and high level of catalytic efficiency. At the same time, there exist some problems, e.g. the instability of enzyme structures, sensitivity to process conditions and their purification cost is high. Fine particles have been used for enzyme stabilization due to their beneficial high surface-to-volume ratio. Enzymes immobilized on fine particles may work at a broader pH, temperature and salinity range than the native enzymes. Ethyl cellulose and poly(lactic co-glycolic acid) carrier particles were prepared by nano spray drying and used for immobilizing horseradish peroxidase enzyme (HRP) by cross-linking. The optimal condition for immobilization was investigated. Fixed enzyme showed increased activity in TRIS buffer. The activity of the immobilized enzyme was enhanced at acidic and alkaline pH.

In Vitro and In Vivo Evaluation of Nanoparticles Prepared by Nano Spray Drying for Stomach Mucoadhesive Drug Delivery

According to a World Health Organization report published in 2010, 346 million people worldwide have diabetes; in Saudi Arabia, 16.8% of the population has been diagnosed with type 2 diabetes. Many patients with type 2 diabetes are unable to maintain adequate glycemic control even after receiving recent antidiabetic drugs. A combination of vildagliptin and metformin hydrochloride tablets is available; however, both conventional drugs have a short half-life. The formulation of mucoadhesive nanoparticles for these classes of drugs can be most beneficial, because they release the drug slowly into the gastrointestinal tract and maintain the therapeutic drug concentration. Vildagliptin and metformin hydrochloride were prepared with Carbopol (VMCN) using a Buchi Nano Spray Dryer B-90. The surface morphology was found to be shriveled (due to surface folding), and the average particle size was 437 nm. The percentage drug yield for vildagliptin and metformin hydrochloride in the nanoparticles was 71 ± 0.5% and 74 ± 0.3%, respectively, and the drug content was 84 ± 0.4% and 89 ± 0.4%, respectively. Ex vivo studies of mucoadhesion were 6.9 ± 0.3 h. The percentage of swelling was recorded as 162 ± 4%. In vivo studies of nanoparticles containing vildagliptin and metformin hydrochloride showed that these values were 3.9 and 4.1% at 12 h, respectively.

Formulation and characterization of clozapine and risperidone co-entrapped spray-dried PLGA nanoparticles

In the current study, polylactide-co-glycolide (PLGA) nanoparticles entrapping both clozapine (CLZ) and risperidone (RIS) were formulated by spray-drying using Buchi Nano Spray Dryer B-90 (Flawil, Switzerland). Parameters such as inlet temperature, spray mesh diameter, sample flow rate, spray rate and applied pressure were optimized to produce nanoparticles having desired release profile using both low- and high-molecular weight PLGA polymer. Smallest size nanoparticle of size around 248 nm could be prepared using a 4.0 μm mesh diameter with low-molecular weight polymer. The load of CLZ and RIS was 126.3 and 58.2 μg/mg of polymer particles, respectively. Entrapment efficiency of drugs in PLGA nanoparticles was 94.74% for CLZ and 93.12% for RIS. Both the drugs released continuously from the nanoparticle formulations. PLGA nanoparticles formulated using low-molecular weight polymer released around 80% of the entrapped drug over 10 days of time. Nature of drug inside polymer particles was amorphous, and there was no chemical interaction of CLZ and RIS with polymer. Polymeric nanoparticles were found to be non-toxic in nature using PC12 cell line. This nanospray drying process proved to be suitable for developing polymeric nanoformulation delivering dual drugs for the treatment of Schizophrenia.

Nano spray-dried pyrazinamide-l-leucine dry powders, physical properties and feasibility used as dry powder aerosols

Objective: The aim of this study was to investigate the effect of adding l-leucine and using an ethanolic solvent on the physicochemical properties and aerodynamic behavior of nano spray-dried pyrazinamide (PZA)-l-leucine powders.Materials and methods: A nano spray dryer was employed to prepare PZA-l-leucine powders. The physicochemical properties were evaluated using a scanning electron microscope (SEM), differential scanning calorimetry and X-ray diffraction. The Andersen cascade impactor was used to evaluate the in vitro aerosolization performance of the sprayed powders.Results and discussion: The incorporation of l-leucine at 10% improved the percentage fine particle fraction (%FPF) in all ethanolic solvent formulations by up to nearly twofold (20.0–23.4%) compared to the normal spray-dried PZA of (8.8–13.0%). Changes in the particle density and morphology were also observed. The dense solid particles of PZA were completely converted to bulk hollow particles with a thin shell by increasing the l-leucine content up to 50%. Higher ethanol concentration resulted in larger dimensions of the hollow particle but did not directly affect the aerosolization performance. The co-spray dried PZA with 20% l-leucine in a 10% ethanol feed solvent gave the best aerosolization performance (FPF = 33.0%).Conclusions: The co-spray dried PZA with a suitable l-leucine content using a nano spray drying technique could be applied to formulate the PZA DPI.

Transforming large molecular weight pectin and chitosan into oral protein drug nanoparticulate carrier

Polymeric nanoparticle formation is characterized by high risks of premature drug leaching and low drug encapsulation efficiency. This is aggravated by slow nanoparticle formation by large molecular weight polymers due to their slow diffusion kinetics in the reaction medium. This study investigated model protein drug insulin encapsulation by large molecular weight pectin and chitosan. The nanoparticles were prepared through pectin–chitosan coacervation and when necessary, together with pectin or chitosan crosslinking by calcium or tripolyphosphate ions in the same process. The formed particles were nanospray-dried when required. The size, zeta potential, morphology, drug content, drug association efficiency, polymer–polymer and drug-polymer interaction in particulate matrix were examined. The pectin–chitosan nanoparticles were able to encapsulate insulin substantially only if these nanoparticles were formed with rapid particle aggregation into micromatrices as a result of particle surfaces attracting the oppositely charged polymer chains via crosslinking as well as coacervation processes. The particulate aggregation level of micromatrices can be reduced via nanospray drying. Small discrete nanoparticles were obtainable from micromatrices.

Encapsulation of folic acid in food hydrocolloids through nanospray drying and electrospraying for nutraceutical applications

In this work, two different technologies (electrospraying and nanospray drying) were evaluated for the encapsulation of folic acid using both a whey protein concentrate (WPC) matrix and a commercial resistant starch. The morphology of the capsules, molecular organization of the matrices upon encapsulation, encapsulation efficiency, and stability of the folic acid within the capsules under different storage conditions and upon thermal exposure were studied. Results showed that spherical nano-, submicro- and microcapsules were obtained through both techniques, although electrospraying led to smaller capsule sizes and to an enhanced control over their size distribution. Greater encapsulation efficiency was observed using WPC as encapsulating matrix, probably related to interactions between the protein and folic acid which favoured the incorporation of the bioactive. The best results in terms of bioactive stabilization in the different conditions assayed were also obtained for the WPC capsules, although both materials and encapsulation techniques led to improved folic acid stability, especially under dry conditions.

Facile fabrication and characterization of chitosan-based zinc oxide nanoparticles and evaluation of their antimicrobial and antibiofilm activity

The present investigation deals with the facile synthesis and characterization of chitosan (CTS)-based zinc oxide (ZnO) nanoparticles (NPs) and their antimicrobial activities against pathogenic microorganisms. ZnO–CTS NPs were synthesized through two different methods: nano spray drying and precipitation, using various organic compounds (citric acid, glycerol, starch and whey powder) as stabilizers. Both the synthesis methods were simple and were devoid of any chemical usage. The detailed characterization of the NPs was carried out using UV–Vis spectroscopy, dynamic light scattering particle size analysis, zeta potential measurements and scanning electron microscopy, which confirmed the fabrication of NPs with different shapes and sizes. Antimicrobial assay of synthesized ZnO–CTS NPs was carried out against different pathogenic microbial strains (Candida albicans, Micrococcus luteus and Staphylococcus aureus). The significant (p < 0.05) inhibition of growth was observed for both M. luteus and S. aureus with ZnO–CTS NPs (with a concentration ranging from 0.625 to 0.156 mg/ml) as compared to control treatment. ZnO–CTS NPs also showed significant biofilm inhibition activity (p < 0.05) against M. luteus and S. aureus. The study demonstrated the potential of ZnO–CTS NPs as antimicrobial and antibiofilm agents.

The development of dimple-shaped chitosan carrier for ethambutol dihydrochloride dry powder inhaler

Objective: In this study, a dimple-shaped chitosan carrier was developed for delivering the antituberculosis drug ethambutol dihydrochloride (EDH) from a dry powder inhaler (DPI) to the lungs.Materials and methods: Nanosized drug particles were prepared using nanospray drying. The microsized carrier was developed from a chitosan solution by spray drying. Five formulations were prepared by physically mixing the drug and carrier in different ratios. The physico-chemical properties of the formulations were analyzed using scanning electron microscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy, ultracentrifugation and a cascade impactor.Result and discussion: The EDH size was 222 nm and the chitosan carrier size was 1.2 µm. Five formulations, i.e. 1:2, 1:2.5, 1:3.3, 1:5 and 1:10 w/w of the EDH to chitosan carrier were prepared by physical mixing. The chitosan carrier was spherical in shape with a dimpled surface and this provided shallow cavities to which the drug was bound, both within its grooves as well as on its surface. The median adhesion force (50% of drug detachment) for formulations #1 to #5 was between 122 and 993 µN. The mass median aerodynamic diameter of the EDH was between 2.3 and 2.7 μm, with the fine particle fractions (aerosolized particles less than 4.4 μm) of 32–42% of the nominal dose.Conclusion: We suggest that ethambutol dihydrochloride mixed with a chitosan carrier was suitable for use in a dry powder inhaler for controlling tuberculosis especially in minimizing the risk of multidrug resistant tuberculosis and the possible side effects from EDH.

Solid phospholipid nano-particles: Investigations into formulation and dissolution properties of griseofulvin

Solid phospholipid (PL) nanoparticles with griseofulvin (GRIS) as a model drug were prepared by co-spray drying. Their dissolution properties were compared with formulations containing the physical blends of the native crystalline drug and excipient materials, and physical blends of the spray dried materials. Co-spray drying was performed from ethanol+water solutions (80+20) using Büchi Nano Spray Dryer B-90. Dissolution profiles in phosphate buffer (PBS), simulated intestinal fluids (fasted state simulated intestinal fluid (FaSSIF)) and pancreatin containing media (PAN) were studied. It was found that the influence of PL on the dissolution profile was affected by both the solid state of the drug formulation and the dissolution medium: the co-SD formulations showed the fastest release in all media. The amount of GRIS dissolved after 5h increases by a factor of 7 for the co SD as compared to physical blend of native materials in PBS, and a factor of 4 in FaSSIF respectively. Surprisingly, in contrast to PBS, dissolution rate in FaSSIF decreased with increasing the PL content. All the pancreatin containing media showed a decrease in dissolution rate and extent independently of the processing methods due to an incompatibility between GRIS and PAN.

Nanospray drying as a novel technique for the manufacturing of inhalable NSAID powders.

The aim of this research was to evaluate the potential of the nanospray drier as a novel apparatus for the manufacturing of a dry powder for inhalation containing ketoprofen lysinate, a nonsteroidal anti-inflammatory drug able to control the inflammation in cystic fibrosis patients. We produced several ketoprofen lysinate and leucine powder batches by means of nanospray dryer, studying the influence of process parameters on yield, particle properties (size distribution and morphology), and, mainly, aerodynamic properties of powders. Micronized particles were prepared from different hydroalcoholic solutions (alcohol content from 0 to 30% v/v) using ketoprofen in its lysine salt form and leucine as dispersibility enhancer in different ratios (from 5 to 15% w/w) with a total solid concentration ranging from 1 to 7% w/v. Results indicated that the spray head equipped with a 7 µm nozzle produced powders too big to be inhaled. The reduction of nozzle size from 7 to 4 µm led to smaller particles suitable for inhalation but, at the same time, caused a dramatic increase in process time. The selection of process variables, together with the nozzle pretreatment with a surfactant solution, allowed us to obtain a free flowing powder with satisfying aerosol performance, confirming the usefulness of the nanospray drier in the production of powder for inhalation.

Nano spray drying of alkaline phosphatase with β-cyclodextrin and l-leucine for inhalation

Nano spray drying of alkaline phosphatase with β-cyclodextrin and l-leucine for inhalation

Spray Drying of Aqueous Salbutamol Sulfate Solutions Using the Nano Spray Dryer B-90—The Impact of Process Parameters on Particle Size

In order to prepare spherical salbutamol sulfate particles of adjustable size, a Nano Spray Dryer B-90 was employed. A 33 full-factorial design was used to investigate the influence of process parameters (mesh size, feed concentration, and drying air temperature) on particle size (median size and width of the particle size distribution), amount of product produced per time, and product yield. The median particle size was significantly influenced by all three factors of the statistical design. Within the design space studied, particle sizes of 1.0 to 6.4 µm were obtained. The width of the particle size distribution (span) increased with increasing mesh sizes. All particles with a particle size greater than 2.4 µm showed a bimodal particle size distribution. Generally, larger mesh sizes as well as higher concentrations led to an increase in the amount of product prepared per time. The corresponding values observed were from 0.4 to 75.8 mg/min. The product yield was independent of the process parameters studied. All products were amorphous after spray drying and were stable up to a relative humidity of 60% at a temperature of 25°C.

Pharmaceutical suspension containing both immediate/sustained-release amoxicillin-loaded gelatin nanoparticles: preparation and in vitro characterization

Pharmaceutical suspension containing oral dosage forms delivering both immediate-release and sustained-release amoxicillin was developed as a new dosage form to eradicate Helicobacter pylori. Amoxicillin-loaded gelatin nanoparticles are able to bind with the mucosal membrane after delivery to the stomach and could escalate the effectiveness of a drug, providing dual release. The objective of this study was to develop amoxicillin nanoparticles using innovative new technology – the Büchi Nano Spray Dryer B-90 – and investigate such features as drug content, particle morphology, yield, in vitro release, flow properties, and stability. The nanoparticles had an average particle size of 571 nm. The drug content and percentage yield was 89.2% ± 0.5% and 93.3% ± 0.6%, respectively. Angle of repose of nanoparticle suspension was 26.3° and bulk density was 0.59 g/cm3. In vitro drug release of formulations was best fitted by first-order and Peppas models with R2 of 0.9841 and 0.9837 respectively; release profile was 15.9%, while; for the original drug, amoxicillin, under the same conditions, 90% was released in the first 30 minutes. The nanoparticles used in this study enabled sustained release of amoxicillin over an extended period of time, up to 12 hours, and were stable for 12 months under accelerated storage conditions of 25°C ± 2°C and 60% ± 5% relative humidity.

Carbopol 934-P Loaded with Vildagliptin for Diabetic Delivery: In Vitro and In Vivo Evaluation of Nanoparticles

Vildagliptin-loaded mucoadhesive nanoparticles using Carbopol 934 P (CVN) as mucoadhesive polymer were prepared by Buchi Nano Spray Dryer to retain the drug in the stomach for a prolonged period of time and to provide sustainable release. The morphological properties of the nanoparticles were studied by scanning electron microscopy and found to have smoother surface with shriveled shape. Drug loading and the percentage recovery werefound to be 89.2 ± 0.5 and 96 ± 0.4 respectively. Bimodal particle size distribution with a mean of 355.8 nm and 80.15 nm was noticed. Angle of repose for CVN particles was relatively good with θ < 32.4°. The percent swelling of CVN formulation was found to be 181±9%. In vivo studies in rats suggest that the vildagliptin was retained in the gastrointestinal tract(GIT) for prolonged period of time (~12 h) and standard group was reduced significantly (~3 h). Stability studies witnessed no changes when stored at 3-5°C or 15 – 25°C, except that the agglutinative phenomenon which was observed at 37°C and RH 75%. This study validates the mucoadhesive nanoparticles as one of the most appropriate drug delivery approaches for the effective delivery of vildagliptin. Keywords: Nanoparticles, vildagliptin, spraydrying, diabetic, carbopol, shriveled.