Formulation Of Drug Delivery System Research Articles

Formulation of a Self-Nanoemulsifying Drug Delivery System of Buckwheat Flavonoids and Evaluation of Its Antimicrobial Activity.

This study was aimed at constructing a self-nanoemulsifying drug delivery system of buckwheat flavonoids and evaluating its antimicrobial activity. The construction of the nanoemulsion followed a pseudo-ternary phase diagram, and its particle properties (particle size, zeta potential, and surface morphology) and physicochemical parameters (turbidity, surface tension, pH value, conductivity, encapsulation efficiency, and stability) were evaluated. The antimicrobial potential of buckwheat flavonoids nanoemulsion was determined against Staphylococcus aureus, Escherichia coli, and Candida albicans and compared to the buckwheat flavonoids suspension. The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) exhibited that the antimicrobial activity of the nanoemulsions and suspension increased while enhancing the drug concentration, and the antimicrobial activity of nanoemulsion was significantly higher than that of the suspension against those three bacteria. Agar disc diffusion test demonstrated that the inhibition zone diameter of the suspension was about 50% of the nanoemulsion against three bacteria. The time killing assay indicated that the IC50 of the nanoemulsion was significantly lower than that of the suspension. These results indicate that nanoemulsion is a promising drug delivery system, which can improve the antimicrobial activity of buckwheat flavonoids.

SNEDDS Formulation of Black Cumin Seed Oil using Tween 80 and Sorbitol as a Surfactant and Cosurfactant

Black cumin seed oil has many benefits. One of which is as an anticancer, it can be used as an opportunity to develop drugs that utilizes the black cumin seed oil. A method to improve the stability and absorption of the drug in the body is within the formulation of Self Nano Emulsifying Drug Delivery System (SNEDDS). This study aims to determine whether the black cumin seed oil can be made into SNEDDS formula with tween 80 and sorbitol as a surfactant and cosurfactant along with the establishment for the optimal formula. SNEDDS formula of black cumin seed oil was optimized using SLD method by DX.10 software. SNEDDS formula was made using tween 80 as surfactant and sorbitol as cosurfactant. Previously carried out with the manufacturing of a trial formula to determine the lower and upper value of each component, then 14 formulas were made based on DX.10. The formula were evaluated for transmittance percentage in 650 nm wavelength and emulsification time of 37oC. Results of the tests included in DX10 is to obtain the optimal formula. The optimal formula was validated by t-test and evaluated for droplet size, zeta potential, and stability test of nanoemulsion in artificial gastric fluid (AGF) and artificial intestinal fluid (AIF) for 4 hours. The results showed that the proportion of 13% black cumin seed oil, 60% tween 80 and 27% sorbitol is able to establish the optimal SNEDDS formula of black cumin seed oil. Transmittan value of the optimal formula was 92% with the emulsification time of 56 seconds, SNEDDS black cumin seed oil droplet size of 21.5 nm, zeta potential value -31.5 mV and nanoemulsion stable in the AIF and AGF.

A Complete Review on Mucoadhesive Buccal Tablets

Drug actions can be improved by novel drug delivery system, such as mucoadhesive system. Mucoadhesive drug delivery systems interact with the mucus layer covering the mucosal epithelial surface, and mucin molecules and prolongs the residence time of the dosage form at the site of application. Bio adhesion may be defined as the state in which two materials, at least one of which is of a biological nature, are held together for extend periods of time by interfacial forces. Buccal mucosa is the preferred site for both systemic and local drug action. The mucosa has a rich blood supply and it relatively permeable. Buccal trans mucosal delivery helps to bypass first- pass metabolism by allowing direct access to the systemic circulation through the internal jugular vein. This article briefly describes. Introduction to mucoadhesive drug delivery system, structure and function of oral mucosal membrane, buccal drug delivery and mucoadhesive property, theories and mechanism of mucoadhesion, mechanism to increase drug delivery through buccal route, buccal drug delivery system formulation design, characterization of buccal tablet, evaluation of buccal tablet.

Formulation, characterization, and in-vivo evaluation of Zaltoprofen self-microemulsifying drug delivery system

Purpose 2-(10,11-Dihydro-10-oxodibenzo [b,f] thiepin-2-yl) propionic acid (Zaltoprofen) is classified as a BCS class II anti-inflammatory drug, having low solubility and less bioavailability. Methods This study describes the development and characterization of self-micro emulsifying drug delivery system (SMEDDS) of the poorly water-soluble compound Zaltoprofen that resulted in improved aqueous solubility, dissolution, and in-vivo oral absorption. The solubility of Zaltoprofen was determined in various vehicles, including oils, surfactants, and co-surfactants. Pseudo-ternary phase diagrams were constructed to identify the most efficient self-emulsification region. The optimized SMEDDS used for Zaltoprofen formulations contained 80% mixtures of surfactant:co-surfactant Labrasol:Cremophor RH 40 (4:1), and 20% of oil, ethyl oleate. Further, SMEDDS was characterized by particle size, zeta potential, dissolution studies, and anti-inflammatory activity. Results The Zaltoprofen-SMEDDS rapidly formed fine oil-in-water microemulsion, which was thermodynamically stable, having an average particle size of 451.3 ± 3.2 nm. The in-vitro dissolution rate of Zaltoprofen from SMEDDS was significantly higher (p<.01) compared to marketed tablets in 0.1N HCL and pH 4.5 buffer. SMEDDS showed highly significant inhibition (p<.01) of inflammation in rat paw edema compared to the drug. Conclusions The study demonstrated that the self-micro emulsifying system poses a promising strategy for developing hydrophobic compounds with low oral bioavailability.

Electrospun PVP/PVA Nanofiber Mat as a Novel Potential Transdermal Drug-Delivery System for Buprenorphine: A Solution Needed for Pain Management

Over the past several decades, the formulation of novel nanofiber-based drug-delivery systems has been a frequent focus of scientists around the world. Aiming to introduce a novel nanofibrous transdermal drug-delivery system to treat pain, the nanofiber mats of buprenorphine-loaded poly (vinyl pyrrolidone) (Bup/PVP) and buprenorphine-loaded poly(vinyl alcohol)/poly(vinyl pyrrolidone) (Bup/PVP/PVA) were successfully fabricated by the electrospinning process for transdermal drug delivery. Similarly, PVP and PVP/PVA nanofibers were fabricated in the same conditions for comparison. The viscosity and electrical conductivity of all electrospinning solutions were measured, and nanofiber mats were characterized by scanning electron microscopy (SEM), atomic force microscopy (AFM), Fourier transform infrared (FT-IR) spectroscopy and contact angle analysis. The conductivity of PVP and PVP/PVA solutions showed a considerable increase by the addition of buprenorphine due to the polarity of buprenorphine. SEM images showed a smooth, fine and porous nanofibrous structure without any adhesion or knot for all of the samples. The contact angle analysis showed the increased hydrophilicity and wettability of PVP/PVA and Bup/PVP/PVA nanofibers compared to PVP and Bup/PVP nanofibers which can be attributed to the addition of PVA. Attenuated total reflectance (ATR) FT-IR results confirmed that the electrospinning process did not affect the chemical integrity of the drug. For the modification of the drug release rate, the cross-linking of nanofiber mats was carried out using glutaraldehyde. Drug release measurements using high-performance liquid chromatography (HPLC) analysis demonstrated that Bup/PVP/PVA nanofibers exhibited better physical and chemical properties compared to Bup/PVP. Furthermore, the cross-linking of nanofibers led to an increase in drug release time. Thus, the novel buprenorphine-loaded nanofibers can be efficient biomaterial patches for transdermal delivery against pain improving carrier retention and providing a controlled release of the drug.

Sodium alginate and pectin estimation in raft forming pharmaceuticals by high performance liquid chromatography method

AbstractThe high performance liquid chromatographic (HPLC) method was developed for the combined estimation of sodium alginate and pectin in raft forming pharmaceuticals on C18 column ZORBAX ODS (1.5 cm × 4.6 mm, 5 μm) with UV detection at 378 nm. The assay condition comprised of phosphate buffer pH 7.4 and methanol 60:40% v/v at a flow rate of 1.25 mL/min. The separation of sodium alginate and pectin with good resolution and a retention time less than 8 min was attained. The method was linear over a range of 200–800 μg/mL of sodium alginate and pectin. The regression values obtained from linearity curve of sodium alginate and pectin were 0.9993 and 0.9991, respectively. The retention time of sodium alginate and pectin was 3.931 and 7.470 min, respectively. The percent recovery of sodium alginate and pectin ranged from 94.2–98.5% and 92.1–98.4% respectively. The limit of detection (LOD) and limit of quantification (LOQ) of sodium alginate were found to be 2.443 and 3.129 μg/mL and the LOD and LOQ of pectin were 3.126 and 3.785 μg/mL, respectively. The resolution of sodium alginate and pectin was found in the range of 1.03–1.89 and 1.10–1.91, respectively. This method has been successfully applied to analyze the concentrations of sodium alginate and pectin in raft forming drug delivery systems.

In-Vitro Dissolution and Characterization of Self-Emulsifying Drug Delivery System of Artemisinin for Oral Delivery

Artemisinin is a compound extracted from Artemisia Annua. Artemisinin is used globally as the first-line antimalarial drug. Despite its high efficacy against the malaria parasite, artemisinin has low bioavailability because it has low solubility in water. This present study was conducted to prepare and characterize the self-emulsifying drug delivery system of artemisinin to increase the dissolution profile of artemisinin. The stability of the resulting emulsion was observed visually for 6 hours. Droplet size, polydispersity index, and zeta potential of the emulsion were measured using Nano Particle Analyzer. The optimum formulation was evaluated with the dissolution test and compared with the artemisinin crystal. Several formulations have good stability of the resulting emulsions where no creaming or flocculation was formed during the observation. Droplet sizes of the resulting emulsions ranged from 114.17-247.93 nm and the polydispersity index of the emulsions ranged from 0.35- 0.56. Zeta potential values of the selected formulations were found in the range of -23.23 - -2.33 mV. Fourier Transform Infrared Spectroscopy spectra of self-emulsifying drug delivery system showed the presence of artemisinin in the formulation with lactone and peroxide peaks. The dissolution of artemisinin in the self-emulsifying drug delivery system was significantly increased compared to artemisinin crystal. Artemisinin was released up to 98,6 %in 150 minutes in self-emulsifying drug delivery system formulation.

Physical properties of microspheres prepared by blending poly(lactide-co-glycolide) and poly lactide

In the present study, ~2.0-μm microspheres of blended poly(lactide-co-glycolide) (PLGA) and poly lactide (PLA), both are biodegradable and biocompatible, were prepared either through a preparation technique for particles using a microhomogenizer or membrane emulsification technique. To understand the potential of the drug delivery system (DDS) formulation, fundamental physical properties, degradation and drug release studies on microspheres prepared using two particle preparation techniques were analysed. The PLGA/PLA particles prepared using the microhomogenizer were polydisperse or irregular-shaped, but the particles prepared using the membrane emulsification technique were very monodisperse and spherical. Increasing the PLA fraction in PLGA/PLA microspheres allowed control over the degradation of the prepared particles. Furthermore, such microspheres could also be used for the controlled drug release behaviour of particles. The particles prepared using the membrane emulsification technique exhibited better controlled drug releasing behaviour than those prepared using the microhomogenizer. From the above, this study revealed that PLGA/PLA microspheres prepared using the membrane emulsification method were advantageous for the study of DDS formulations.

Self-Nanoemulsifying Drug Delivery System of Genkwanin: A Novel Approach for Anti-Colitis-Associated Colorectal Cancer.

PurposeThe aim of the present study was to develop an optimized Genkwanin (GKA)-loaded self-nanoemulsifying drug delivery system (SNEDDS) formulation to enhance the solubility, intestinal permeability, oral bioavailability and anti-colitis-associated colorectal cancer (CAC) activity of GKA.MethodsWe designed a SNEDDS comprised oil phase, surfactants and co-surfactants for oral administration of GKA, the best of which were selected by investigating the saturation solubility, constructing pseudo-ternary phase diagrams, followed by optimizing thermodynamic stability, emulsification efficacy, self-nanoemulsification time, droplet size, transmission electron microscopy (TEM), drug release and intestinal permeability. In addition, the physicochemical properties and pharmacokinetics of GKA-SNEDDS were characterized, and its anti-colitis-associated colorectal cancer (CAC) activity and potential mechanisms were evaluated in AOM/DSS-induced C57BL/6J mice model.ResultsThe optimized nanoemulsion formula (OF) consists of Maisine CC, Labrasol ALF and Transcutol HP in a weight ratio of 20:60:20 (w/w/w), in which ratio the OF shows multiple improvements, specifically small mean droplet size, excellent stability, fast release properties as well as enhanced solubility and permeability. Pharmacokinetic studies demonstrated that compared with GKA suspension, the relative bioavailability of GKA-SNEDDS was increased by 353.28%. Moreover, GKA-SNEDDS not only significantly prevents weight loss and improves disease activity index (DAI) but also reduces the histological scores of inflammatory cytokine levels as well as inhibiting the formation of colon tumors via inducing tumor cell apoptosis in the AOM/DSS-induced CAC mice model.ConclusionOur results show that the developed GKA-SNEDDS exhibited enhanced oral bioavailability and excellent anti-CAC efficacy. In summary, GKA-SNEDDS, using lipid nanoparticles as the drug delivery carrier, can be applied as a potential drug delivery system for improving the clinical application of GKA.

Biological Evaluation of Oil-in-Water Microemulsions as Carriers of Benzothiophene Analogues for Dermal Applications.

During the last decade, many studies have been reported on the design and formulation of novel drug delivery systems proposed for dermal or transdermal administration. The efforts focus on the development of biocompatible nanodispersions that can be delivered to the skin and treat severe skin disorders, including cancer. In this context, oil-in-water (O/W) microemulsions have been developed to encapsulate and deliver lipophilic bioactive molecules for dermal application. An O/W biocompatible microemulsion composed of PBS buffer, Tween 80, and triacetin was assessed for its efficacy as a drug carrier of DPS-2, a lead compound, initially designed in-house to inhibit BRAFV600E oncogenic kinase. The system was evaluated through both in vitro and ex vivo approaches. The cytotoxic effect, in the presence and absence of DPS-2, was examined through the thiazolyl blue tetrazolium bromide (MTT) cell proliferation assay using various cell lines. Further investigation through Western blotting revealed that cells died of necrosis. Porcine ear skin was used as a skin model to evaluate the degree of permeation of DPS-2 through skin and assess its retention. Through the ex vivo experiments, it was clarified that encapsulated DPS-2 was distributed within the full thickness of the stratum corneum (SC) and had a high affinity to hair follicles.

A comprehensive study of the basic formulation of supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) of albendazolum

Albendazolum (ABZ) is a BCS class II drug. It has challenging biopharmaceutical properties, which include poor solubility and dissolution rate. These properties have laid the ground for developing a supersaturated self-nanoemulsifying drug delivery system (S-SNEDDS) to form oil-in-water nanoemulsion in situ to improve the oral bioavailability of ABZ. Based on the ABZ solubility, emulsifying ability, and stability after dispersion in an aqueous phase, an optimal self-nanoemulsifying drug delivery system (SNEDDS) consisting of oleic acid, Tween® 20, and PEG 600 (X:Y:Z, w/w) was identified, having 10% (w/w) hydroxypropyl methylcellulose (HPMC) E15 lv as its precipitation inhibitor. The optimized system possessed a small mean globule size value (89.2 nm), good dispersion properties (polydispersity index (PDI): 0.278), and preserved the supersaturated state of ABZ. S-SNEDDS was transformed into solid supersaturated self-nanoemulsifying drug delivery systems (SS-SNEDDS) using microcrystalline cellulose as a solid material. The developed S-SNEDDS were characterized for globule size, pH, turbidity, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and flow properties. The data obtained from the results suggest that this S-SNEDDS formulation can enhance the solubility and oral bioavailability of ABZ for appropriate clinical application.

A Recent Update on Formulation and Development of Gastro-Retentive Drug Delivery Systems

Oral route has been the most convenient and accepted route of drug delivery. Owing to tremendous curative benefits of the oral controlled release dosage forms are being preferred as the interesting topic in pharmaceutical field to achieved improved therapeutics advantages. Gastro retentive drug delivery system is novel drug delivery systems which has an upper hand owing to its ability of prolonged retaining ability in the stomach and thereby increase gastric residence time of drugs and also improves bioavailability of drugs. Concept of novel drug delivery system arose to overcome the certain aspect related to physicochemical properties of drug molecule and the related formulations. In this context, various gastro retentive drug delivery systems have been used to improve the therapeutic efficacy of drugs that have a narrow absorption window, are unstable at alkaline pH, are soluble in acidic conditions, and are active locally in the stomach. Concept of novel drug delivery system arose to overcome the certain aspect related to physicochemical properties of drug molecule and the related formulations. Various approaches are currently used including gastro retentive floating drug delivery systems, swelling and expanding system, polymeric bio adhesive systems, modified shape systems, high density system and other delayed gastric emptying devices. Moreover, future perspectives on this technology are discussed to minimize the gastric emptying rate in both the fasted and fed states. The present review briefly addresses the physiology of the gastric emptying process with respect to floating drug delivery systems. The purpose of this review is to bring together the recent literature with respect to the method of preparation, and various parameters affecting the performance and characterization of floating microspheres. Attempt has been made to summarize important factors controlling gastro retentive drug delivery systems. Overall, this review may inform and guide formulation scientists in designing the gastro retentive drug delivery system.

Acute Oral Toxicity Evaluation of Andrographolide Self-Nanoemulsifying Drug Delivery System (SNEDDS) Formulation.

Context:Andrographolide (AND) is an active compound of well-known medicinal plant Andrographis paniculata. It has been widely published for various activities. AND is difficult to develop into dosage form due to its poor solubility and bioavailability. This problem could be solved by using self-nanoemulsifying drug delivery system (SNEDDS) for its formulation. However, the increase of bioavailability might result in potential toxicity as a large amount of drug is absorbed.Aims:The aim of this study is to evaluate the acute potential toxicity using Organization for Economic Cooperation and Development (OECD) test: 401 methods.Subjects and Methods:The OECD 401 method employs groups of animals treated by a single dose or repeated dose (<24 h) of the drug with three variances of doses. In this study, thirty male Wistar rats were divided into five groups which consisted two groups of control and three groups of AND SNEDDS formulation (500, 700, and 900 mg/kg body weight [BW], respectively). Intensive observation of toxicity symptom was performed during the first 30 minutes followed by periodic observation for 14 days. Posttermination, histopathological examination of the liver and kidney was conducted to confirm the toxicity symptoms. To determine the level of toxicity, the lethal dose 50 (LD50) value was calculated at the end of the study.Results:The result showed that all groups presented similar toxicological symptoms such as salivation, lethargy, and cornea reflex. However, based on histopathological examination, there were abnormalities, but still in an early stage. The toxicological symptom that emerged seems related to the SNEDDS formulation with lipophilic properties. Furthermore, the value of LD50 was 832.6 mg/kg BW (po).Conclusions:The AND SNEDDS formulation was slightly toxic in male Wistar rats po.

Advance of Etiologies and Treatments on Schizophrenia

Schizophrenia is a severe psychiatric disorder. Among the globe, almost 70% of people with schizophrenia would experience hallucinations that make them feel insecure and progressively weakened. Etiologies and treatments of this perilous disease, therefore, are supposed to be studied in depth. Although the exact causes are still unknown, scientists highly suggest that this disorder results from the combination of genes and environments. For genetic influences, genes such as NR3C2, Dysbindin-1 (DTNBP1), Neuritin-1 (NRN1), KPNB3, and KPNA3 play insignificant roles in the development of schizophrenia. For environmental influences, researchers collected data from different aspects to infer the causes of schizophrenia. The reasons, including season of birth, urbanization, are not related to schizophrenia causation. Furthermore, if pharmacological interventions such as chlorpromazine, followed by some psychotherapy at an early stage, schizophrenia has a chance of being cured and not relapsing. Many drugs on the market target G-protein-coupled receptors. To improve their bioavailability, a new technique called lipid-based self-nanoemulsifying drug delivery systems formulations assists with the absorption of them.

Formulation and Evaluation of High-Density Gastro Retentive Drug Delivery Systems of Norfloxacin

Formulation and Evaluation of High-Density Gastro Retentive Drug Delivery Systems of Norfloxacin

Recent Advances in Microfluidics for the Preparation of Drug and Gene Delivery Systems.

Drug delivery systems (DDSs) have great potential for improving the treatment of several diseases, especially microbial infections and cancers. However, the formulation procedures of DDSs remain challenging, especially at the nanoscale. Reducing batch-to-batch variation and enhancing production rate are some of the essential requirements for accelerating the translation of DDSs from a small scale to an industrial level. Microfluidic technologies have emerged as an alternative to the conventional bench methods to address these issues. By providing precise control over the fluid flows and rapid mixing, microfluidic systems can be used to fabricate and engineer different types of DDSs with specific properties for efficient delivery of a wide range of drugs and genetic materials. This review discusses the principles of controlled rapid mixing that have been employed in different microfluidic strategies for producing DDSs. Moreover, the impact of the microfluidic device design and parameters on the type and properties of DDS formulations was assessed, and recent applications in drug and gene delivery were also considered.

Formulation and evaluation of self-nanoemulsifying drug delivery system of brigatinib: Improvement of solubility, in vitro release, ex-vivo permeation and anticancer activity

The aim of this study was to develop a novel self-nanoemulsifying drug delivery system (SNEDDS) of brigatinib, a poorly soluble anticancer drug, so as to improve its solubility, in vitro release, ex-vivo permeation and anticancer activity. Components of SNEDDS were screened on the basis of maximum solubility of brigatinib. Oleic acid, Tween 20 & diethylene glycol monoethylether were selected as oil phase, emulsifier and co-solvent respectively. Various brigatinib-SNEDDS were developed by spontaneous, low energy, simple mixing method. Developed SNEDDS were optimized on the basis of self-emulsifying capacity, globule size, size distribution, thermodynamic stability and capacity to solubilize maximum amount of brigatinib. The optimized SNEDDS was characterized for physicochemical evaluations such as viscosity, conductivity, pH and refractive index in addition to morphological evaluation of globule size and shape by transmission electron microscopy. The optimized SNEDDS exhibited approximately 205-fold enhancement in the saturation solubility of the brigatinib that resulted in improved in vitro release of drug from SNEDDS as compared to pure drug (P < 0.01). The ex-vivo permeation of brigatinib-SNEDDS across rat intestinal sacs was also improved as compared to pure drug (P < 0.01). The cytotoxic activity of brigatinib-SNEDDS against A549 human lung cancer cell lines during MTT assay were significantly improved as compared to pure brigatinib probably due to improved permeability of the SNEDD loaded brigatinib.

Formulation and evaluation of a solid self-emulsifying drug delivery system containing cefuroxime axetil

Formulation and evaluation of a solid self-emulsifying drug delivery system containing cefuroxime axetil

Understanding the Concept of Chronotherapeutics in the Management of Diabetes Mellitus.

The circadian rhythms have been controlled with the aid of a circadian clock in the hypothalamus region, which is known as the suprachiasmatic nucleus. Chronotherapeutics, a branch of pharmacotherapeutics, plays a mandatory role in the treatment of various disorders, such as delivering the drug in the correct schedule, correct site, and correct extent and provides benefit to the patients. The chronopharmacological aspects are very much important in the treatment of diabetes mellitus during daytime as the patients' timing of daily activities of body and medicine treatment has an impact on the increase in the glucose levels in the blood. This leads to the fact that the increased risk of obesity and diabetes gets worse, ultimately increasing the rates of cardiovascular diseases and deaths. According to a medical saviour who works on the problems related to diabetes, the level of glucose in plasma changes independently as regard to eating habits and use of insulin and medicines. People suffering from dawn phenomenon are difficult to manage, hence, the basic aim is to detect the functioning of the biological clock of human body and its chronotherapeutic effect on human beings that increases the therapeutic effects and reduces side effects. Keeping these points in mind, an attempt has been made in the present review to discuss the role of chronotherapy in the management of diabetes, various techniques used in formulation and design of chronotherapeutic drug delivery systems and regulatory issues related to chronotherapeutics.

Colitis-targeted hybrid nanoparticles-in-microparticles system for the treatment of ulcerative colitis

Nanoparticle (NP)-based drug delivery systems accumulate in the disrupted epithelium of inflamed colon tissue in ulcerative colitis. However, premature early drug release and uptake or degradation of NPs during their passage through the harsh gastric or intestinal environment compromise their therapeutic outcomes. This study aimed to develop an advanced colitis-targeted hybrid nanoparticles-in-microparticles (NPsinMPs) drug delivery system to overcome the aforementioned challenges. First, sustained drug releasing poly(lactic-co-glycolic acid) NPs were generated and further encapsulated in pH-sensitive Eudragit FS30D MPs to ensure complete drug protection in a gastric-like pH and for selective delivery of NPs to the colon. SEM and confocal microscopy for the NPsinMPs revealed successful NP encapsulation. NPsinMPs prevented drug release in an acidic gastric-like and intestinal-like pH and presented a sustained release thereafter at an ileal and colonic pH, indicating the degradation of the outer pH-sensitive MPs and release of NPs. Furthermore, in vivo imaging of gastrointestinal tract of a colitis mouse orally administered with fluorescent NPsinMPs revealed higher fluorescence intensities selectively in the colon, demonstrating the release of loaded NPs and their concomitant accumulation at the site of colon inflammation. NPsinMPs markedly mitigated experimental colitis in mice indicated by improved histopathological analysis, decreased myeloperoxidase activity, neutrophils and macrophage infiltration, and expression of proinflammatory cytokines in colonic tissues compared with NP-treated mice. The present results show the successful formulation of an NPsinMP-based drug delivery system and provide a platform to improve NP-based colon-targeted drug delivery through improved protection of encapsulated NPs and their payload in the early small intestine.