Quasi-emulsion Solvent Diffusion Method Research Articles

Microsponges enriched gel for enhanced topical delivery of 5-fluorouracil

This study aimed to develop microsponges based topical gel formulation of 5-Fluorouracil (5-FU) for the treatment of skin cancer with enhanced skin deposition and reduced skin irritation potential. Microsponges were prepared by Quasi-emulsion solvent diffusion method using ethyl cellulose and Eudragit RL 30 D; and was optimised through detailed in vitro characterisation. Brunauer–Emmett–Teller (BET) analysis demonstrated higher surface area (2.4393 m2/g) and pore volume of developed microsponges formulation. Optimised formulation showed better thixotropic and texture properties compared to commercial cream formulation, used as control for comparison purpose. Further, the optimised formulation demonstrated 5.5-fold increase in skin deposition documented via in-vivo local bioavailability study, with significant reduction in skin irritation compared to the commercial formulation. Hence, the developed microsponges based formulation seems to be a viable alternative with enhanced topical delivery of 5-FU as compared to the commercial formulation.

Sulpiride gastro-retentive floating microsponges; analytical study, in vitro optimization and in vivo characterization

Sulpiride (SUL), anti-dopaminergic drug, has a specific site for absorption located in the upper portion of the gastrointestinal tract hence, its oral delivery represents a challenge regarding SUL absorption and bioavailability. So, a gastro-retentive oral platform of SUL was developed to increase its gastric residence time, release SUL at a controlled rate in the stomach and consequently, enable it to reach its specific absorption site. Floating microsponges were prepared via quasi-emulsion solvent diffusion method and characterised for their physico-chemical properties. In addition, Taguchi design of experiment was utilised to optimise some independent variables affecting microsponges performance. The optimised SUL microsponges showed a yield of 79.82 ± 2.37%, an encapsulation efficiency of 89.11 ± 2.28% and in vitro time for floatation of 8.0 h. Additionally, pharmacokinetics were investigated in rabbits and compared with the commercial SUL formulation, Dogmatil® capsules. Optimised SUL microsponges showed a significantly (p < .05) higher Cmax, AUC and 2-fold increase in oral bioavailability compared with the commercial product. Moreover, the optimised SUL microsponges remained present in the stomach up to 8.0 h post administration when viewed via X-ray radiographs in rabbits. It could be concluded that the floating microsponges could be useful as an oral platform to enhance the sulpiride absorption and bioavailability.

Development and Evaluation of Particulate Microcarriers of Adapalene as a Topical Delivery System

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.

Formulation and Evaluation of Copper Nanoparticles Loaded Microsponges

Microsponges become imperative in the field of targeted drug delivery and in other biomedical applications. There was a clamant need for designing microsponges incorporating with green synthesised metal nanoparticles rather than the chemical drug in order to reduce the side effects of the drug and thus increasing the effectiveness of nature of the whole material. It provokes us to design this novel approach of loading copper nanoparticles into the microsponges. Here in this work, microsponges based on ethyl cellulose and polyvinyl alcohol were synthesised by Quasi-Emulsion Solvent diffusion method in which copper nanoparticles procured from Hibiscus rosa-sinensis leaf extract was incorporated. The Loaded microsponges were characterised by High Resolution Scanning Electron Microscopy (HR-SEM) and Particle size distribution Analyzer (PSA). The Drug content and Entrapment Efficiency of the microsponges were found out. The antimicrobial and antioxidant activity of the loaded microsponges were evaluated.

A 32 FULL FACTORIAL DESIGN FOR TOPICAL CONTROLLED RELEASETAZAROTENE MICROSPONGE USING HPMC GEL

Objective: The aim of present work was to the development of control release 0.1% tazarotene microsponge and incorporated into a HPMC K-100M gel.&#x0D; Methods: Drug compatibility with polymer was evaluated by FT-IR spectrum. Tazarotene microsponge was prepared by quasi-emulsion solvent diffusion method. On the basis of preliminary results, 32 full factorial design was employed to study the effect of Eudragit RS-100 conc. (X1) and PVA conc. (X2) on as particle size (Y1), % drug entrapment (Y2) and time required to 80% drug release (Y3). Multiple linear regression analysis, ANOVA and graphical representation of the influence factor by 3D plots were performed by using Sigma plot 11.0. In this study, the following constraints were arbitrarily used for the selection of an optimized batch: particle size&lt;200 µm, drug entrapment&gt;70 %, and time required to 80% drug release&gt;360 min. The optimized formulation was subjected to SEM study. Tazarotene microsponge incorporates in 3% HPMC K-100M gel evaluated for viscosity, pH, drug content, spreadability, In vitro diffusion study, release kinetic study and photostability study.&#x0D; Results: The FT-IR result showed that there was no chemical interaction and SEM photograph indicates that microsponges are spherical and pores. From the results of multiple regression analysis, it was found that all factors had a statistically significant influence on all dependent variables.&#x0D; Conclusion: The optimized formulation of gel release kinetics having good linearity (R2= 0.987) of zero-order kinetic and it was found to be stable in the stability evaluation.

PREPARATION AND EVALUATION OF PARECOXIB MICROSPONGE HYDROGEL SUSTAINED RELEASED TABLET

Microsponges are the polymeric drug delivery systems composed of porous microspheres. They are tiny sponge like spherical particles that consists of myriad of inter-connecting voids within a non-collapsible structure with a large porous surface. The present work is to formulate and evaluate the Parecoxib Microsponge Hydrogel Sustained Release Tablet. The Microsponges of Parecoxib is prepared by Quasi-emulsion solvent diffusion method using Ethyl cellulose and Eudragit RS100 as polymers and Di-butyl phthalate as Plasticizer. And they are characterized for FTIR studies, production yield, particle size analysis, DSC and SEM. The production yield of formulations was from 77.77 to 82.75. FTIR and DSC studies are revealed that the drug and polymer are compatible with each other during preparation. The average diameter of Microsponge is ranged from 536.9 nm to 489.7.&#x0D; Parecoxib Microsponge hydrogel were prepared as sustained release tablets by using sustained release polymers like MCC, Magnesium stearate, Lactose and talc. Preformulation of Microsponge granules were carried out by various parameters and post formulation were carried out by In-vitro dissolution studies, hardness, friability and weight variation tests. Formulation F3 shows good results for the drug release kinetics as controlled release and F6 formulation shows good results for the in-vitro dissolution studies for sustained release.&#x0D; Key words: Microsponge hydrogel drug delivery, Parecoxib, Sustained drug release tablets, quasi emulsion solvent diffusion method.

Formulation and Evaluation of Fluconazole Microsponge using Eudragit L 100 by Quasi Emulsion Solvent Diffusion Method

The aim of the present study is to formulate and evaluate the fluconazole microsponge by using Eudragit L 100. Microsponge was made because they provide controlled as well as target specific release of the drug. Thus study the effect of stirring rate on the formation of microsponge. Microsponge containing Fluconazole were prepared by quasi-emulsion solvent diffusion method at different stirring rate i.e 500, 800, 1000, 1200 and 1500 rpm. Particle size of prepared microsponge was observed in the range of 76.2 to 32.5μm. Scanning electron microscopy revealed the porous, spherical nature of the microsponges. The production yield, entrapment efficiency and drug content were found to be 78.24%, 82.76%, 81.36%. The impact of Drug: Polymer ratio and process variables i.e stirring speed and stirring time on the physical features of microsponges like production yield, mean particle size, entrapment efficiency were examined. It was shown that production yield, drug content and entrapment efficiency was found to be increase with increase in drug polymer ratio while drug: polymer ratio has reverse effect on particle size, as drug: polymer ratio increase, particle size decrease. As the polymer concentration increased, more amount of polymer surrounding the drug, thus increasing the thickness of the wall of the polymer matrix which lead to extended diffusion path and ultimately to lesser drug release or more sustained release. The effect of stirring rate on the morphology of microsponge. The formulation with higher drug to polymer ratio 1:8 (i.e F4) was chosen to investigate the effect of stirring rate on the morphology of microsponges. The dispersion of the drug and polymer within the aqueous phase was found to be dependent on the agitation speed. As the speed was increased the size of microsponges was reduced and the microsponges were found to be spherical and uniform. Keywords: Novel drug delivery system, Microsponges, Eudragit L 100, Fluconazole, Quasi-emulsion solvent diffusion method.

Preparation and Characterization of Itraconazole Microsponges using Eudragit RSPO and Study the Effect of Stirring on the Formation of Microsponges

The purpose of the present study was to prepare and evaluate Itraconazole loaded microsponges using Eudragit for the controlled release of the drug and study the effect of stirring rate on the formation of microsponges. Microsponges containing Itraconazole were prepared by using quasi-emulsion solvent diffusion method at different stirring rate i.e. 500, 800, 1000, 1200 and 1500rpm. Particle size of prepared microsponge was observed in the range of 78.43 to 23.18 µm. Scanning electron microscopy revealed the porous, spherical nature of the microsponges. The production yield, entrapment efficiency, and drug content were found to be 80.88%, 84.53% and 82.89%. The formulation with higher drug to polymer ratio 1:10 (i.e. F5) was chosen to investigate the effect of stirring rate on the morphology of microsponges. As the speed was increased, the particle size of microsponges was reduced and uniform spherical microsponges were formed. As drug polymer ratio increased, Production yield, drug content and entrapment efficiency was found to be increased while drug: polymer ratio has reverse effect on particle size, as drug: polymer ratio increase, particle size decreases. The cumulative percentage drug release upto 8hrs for F5 was 89.54% and the mechanism of drug release from the formulations during the dissolution was determined using the zero order, first order, higuchi equation and Peppas equation. All formulations were best fitted to Zero order and peppas plot. The best formulation F5 follows Zero order release. Keywords: Microsponges, Itraconazole, stirring rate, Quasi-emulsion solvent diffusion method

The NANOSPONGES: AN INNOVATIVE DRUG DELIVERY SYSTEM

For prolonged time there is a delusion for efficacious targeted drug delivery system, but the chemistry hold complex form had made situations thorny, but the development of new colloidal carrier called nanosponges (NSs) likely circumvent these problems. NSs are the nanoporous particles that can entangle a huge range of material and then be engulfed into a suitable formulation depend on the route of administration. They prevent the drug-protein degradation, lengthen the drug release in a controlled manner, and release the medicament to the target site. They can travel around the body and attach on the surface and liberate the drug in a controlled and predictable manner at the specific target site. They are fine aqueous solubility which makes them a bearer for low water-soluble drugs. Drugs having low bioavailability are best suited for this type of carrier system. Both lipophilic and hydrophilic drugs can be included in NSs. Particle size can change from smaller to bigger by varying the amount of crosslinker to the polymer. Various applications of NSs such as recovering bioavailability of active ingredient molecule and delivery of active ingredient into oral, topical, parenteral, and nasal route make them a superior candidate for targeted delivery of drugs. It can be used as a shipper for biocatalysts in the transport and release of enzymes, proteins, vaccines, and antibodies. They can be prepared by different methods such as emulsion solvent diffusion method, melt method, ultrasound-assisted method, Quasi emulsion solvent diffusion method. This analysis is focusing on the advantages, formulation, evaluation, application, and patent report of the NSs.

Three-solvent spherical crystallization method with a model drug: Clopidogrel hydrogen sulfate

A novel three-solvent spherical crystallization method for producing monodisperse spherical particles with potential use in industry has been presented in this work. By combining the advantages of quasi-emulsion solvent diffusion (QESD) and spherical agglomeration (SA) method, the new approach adds another solvent as diffusion agent which can form a partially miscible zone with good and poor solvents in their phase diagram, changing the diffusion driving force into the transformation of composition point of solvent system from immiscible to miscible region in phase diagram of solvents system. This study presents a detailed process and characterization of obtained spheres in terms of size distribution and morphologies by using clopidogrel hydrogen sulfate (CHS) as a model drug. The effects of process parameters on spheres size and morphology are also investigated experimentally. The results show that particles of defined size and morphology can be prepared precisely by tuning the process conditions. Furthermore, the morphologies exhibit a continuous structural transition from polycrystalline to single crystal. This approach overcomes the shortage of QESD requiring large amount of poor solvent, and also breaks through the main difficulty of selecting suitable bridging liquid of SA method. Although CHS is used as model drug, this method is easily generalized to other drugs.

Computational Predictability of Microsponge Properties Using Different Multivariate Models.

The capabilities of principal component regression (PCR) and multiple linear regression (MLR) were evaluated to decipher and predict the impact of formulation and process parameters on the modeled metronidazole benzoate (MB)-ethyl cellulose (EC) microsponge (MBECM) properties. MBECM were prepared by a quasi-emulsion solvent diffusion method. A minimum experimentation was designed using Box-Behnken approach with one center point after initial screening experiments. Data was modeled by principal component analysis (PCA), PCR, and MLR. Two distinct groupings of developed MBECM was observed in initial qualitative PCA as a function of their respective formulation and processing parameters. Group A formulations with low dichloromethane, high PVA, and low stirring speed exhibited larger particle size, lower entrapment efficiency (EE), and lower actual drug content (ADC) than Group B formulations. Optimized quantitative PCR and MLR models demonstrated a linear dependence of particle size and quadratic dependence of EE and ADC on the studied formulation and process parameters. Interestingly, MLR models showed relatively better predictability of the selected MBECM formulation properties when compared with PCR. MBECM were amorphous in nature and spherical shaped. Carbopol® 940 NF based hydrogel of selected MBECM formulation exhibited a prolonged MB release than the commercial MB gel (Metrogyl®), showing no signs of necrosis in the goat mucosa. Thus, a properly designed minimum experimentation coupled with multivariate modeling generated a knowledge-rich target space, which enabled to understand and predict the performance of developed MBECM within a prescribed design space.

Formulation, development and evaluation of Microsponge loaded Topical Gel of Nystatin

Nystatin containing microsponge as active constituent (API) in different formulations by changing the proportions of drug (Nystatin), polymer (ethyl cellulose), emulsifier (Poly vinyl alcohol) were obtained successfully using quasi-emulsion solvent diffusion method. These formulations were studied for particle size and physical characterization. Scanning electron microscopy (SEM) images showed the microsponges porous and spherical in shape. The physical characterization showed that microsponge formulation coded by P6 showed a better loading efficiency and production yield. This microsponge formulation was prepared as gel in carbopol and studied for pH, viscosity, spreadability, drug content, in-vitro release. The microsponge formulation gel, F3 showed viscosity3465.84cps,spreadability of 26.22g cm/s and drug content of 89.65%. The nystatin microsponge gel formulations showed an appropriate drug release profile. F3 released 81.03% of drug at 12 hours. Keywords: Microsponge, Solvent diffusion method, Scanning electron microscope, Nystatin microsponge gel.

Spherical agglomeration to improve dissolution and micromeritic properties of an anticancer drug, Bicalutamide

Bicalutamide (BCT), an anticancer drug, suffers from dissolution rate limited bioavailability and poor micromeritic properties. Spherical crystallization involves the formation of spherical agglomerates with enhanced dissolution properties, obviating the need for further granulation process. The present investigation was focused on spherical agglomeration of BCT by quasi-emulsion solvent diffusion method. All the responses were subjected to principal component analysis to scrutinize the critical attributes. Further for optimization, X1; influence of phase ratio, X2; amount of PEG 6000 and X3; stirring speed on critical dependent variables was studied by employing the Box-Behnken experimental design. The agglomerates exhibited better flow properties, higher bulk density, and improved compressibility compared to pure powder drug. In-vitro release studies revealed enhancement of dissolution properties of poorly soluble BCT. Characterization studies carried out by differential scanning calorimeter and powder X-ray diffractometer revealed crystallinity of drug with decreased intensity in the formulation. Scanning electron microscopy showed spherical shape agglomerates of BCT. The residual solvents were largely below the permitted limits. Spherical agglomerates demonstrated enhanced dissolution properties on account of reduced particle size and partial conversion into amorphous form. Thus, spherical agglomerates of BCT seem to be a promising approach to ameliorate the dissolution properties which might thereby improve its bioavailability.

Dendrimer entrapped microsponge gel of dithranol for effective topical treatment

Dithranol is one of the important topical agents for the treatment of psoriasis, a chronic inflammatory skin disease with aberrant differentiation of keratinocytes. However, its application is troublesome and inconvenient because of its associated side effects, including staining, burning sensation, irritation, and necrotizing effect on the diseased cells as well as on the normal cells. The purpose of the current investigation was to explore the potential of poly(amido) amine (PAMAM) dendrimers in the topical delivery of dithranol through a novel microsponge based gel. Generation-4 (G4) dendrimers were incorporated into the microsponge based gel formulation by quasi-emulsion solvent diffusion method with varying concentration of polymers, and evaluated for the morphology of the formulation, encapsulation efficiency and skin irritation potential. Percentage yield of the formulation was found to be 66.28%, whereas encapsulation efficiency was ranged between 71.33% to 49.21%, and an average particle size was ranged between 28 ± 1.12 μm to 130 ± 1.01 μm. Surface morphology of developed microsponge was confirmed by scanning electron microscopy, revealed micro-porous nature. The optimized microsponge formulation was found to be stable and recorded non-irritant during cutaneous application of the experimental animals. Further, the pharmacokinetic outcomes of study were showed prolong penetration of the drug through the skin, equivalent to the marketed formulation of dithranol. Therefore, it could be conferred that the microsponge formulation of the PAMAM entrapped dithranol can produce prolonged efficacy without producing toxicities to the skin, and thus can effectively be projected in the treatment of diseases like psoriasis.

Development and Characterization of Lornoxicam loaded microsponge gel for Rheumatoid arthritis

Transdermal delivery, a successful novel approach aimed at achieving systematically active level of drug. The drug lornoxicam is a non-steroidal anti-inflammatory drug bearing analgesic, anti-inflammatory, and antipyretic property. The micro sponge technology used to facilitate the controlled release of active drug into the skin in order to reduce the systematic exposure and minimize local cutaneous reactions of active drugs. The main objective of this work was to design and evaluate the gel formation of microsponge entrapped lornoxicam to increase the effectiveness of the treatment. The microsponges were prepared by quasi emulsion solvent diffusion method. The internal phase consisting eudragit RS-100 dissolved in dichloromethane, drug is slowly added to polymer solution with continuous stirring for 4 h, and then mixture was filtered to separate the microsponges. Microsponges was characterized by parameters like scanning electron microscopy, drug content, particle size analysis, compatibility studies using differential scanning calorimetry. Microsponge-loaded gel was characterized by physical parameters of gel, measurement of PH, viscosity study, Drug content study, in-vitro release studies using Franz diffusion cell, cellophane membrane. The prepared gel were subjected to different kinetics models showed that the release data, rheological study, thixotrophy analysis, FT-IR spectral analysis. The release profile of the lornoxicam in the form of microsponges gel was compared with that of pure lornoxicam gel. From the results it can be concluded that microsponges gel LMSG-2 formulation shows drug release in a controlled manner could sustain the drug release over period of 8 hours.

Formulation and In- Vitro Evaluation of Spherical Crystal Agglomerates of Ebastine by Quasi Emulsion Solvent Diffusion Method

Ebastine (EBS) is a poorly water-soluble antihistaminic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS). The aim of the present work was to enhance the solubility, dissolution rate and micromeritic properties of the drug, by formulating it as spherical crystal agglomerates by Quasi Emulsion Solvent Diffusion (QESD) method.&#x0D; Spherical crystal agglomerates (SCAs) were prepared in presence of three solvents dichloromethane (DCM), water and chloroform as a good solvent, poor solvent and bridging solvent respectively. Agglomeration of EBS involved the use of some hydrophilic polymers like polyethylene glycol 4000 (PEG 4000), polyvinyl pyrrolidine K30 (PVP K30), D-?-tocopheryl polyethylene glycol 1000 succinate (TPGS) and ?. cyclodextrin. The pure drug (EBS) and its agglomerates with and without polymers were characterized for their drug content, percentage yield, solubility, in vitro drug release study and micromeritic property as well as by optical microscope, Scanning Electron Microscopy (SEM), FTIR spectroscopic studies, Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD). The results of this work showed that there was a marketed enhancement in the solubility with improvement in dissolution rate, physiochemical properties, decrease in crystallinity and alteration in the crystal habit of the drug especially in presence of polymers. The best results were obtained with formula prepared by the combination of PEG 4000 and B. cyclodextrin in the agglomeration process of (EBS).

Microsponge: An emerging drug delivery strategy.

Microsponges are the spherical particles ranging from 5 to 300 μm in size. These are further made up of clusters of smaller spheres. They are designed for delivering the drug efficiently at a comparatively lesser dose and enhancing the stability, modifying the drug release profile and minimizing the side effects. Microsponge drug delivery system decrease transdermal invasion of the active ingredient into the skin while increasing the time the drug remains on the skin surface or within the epidermis. Preparation of the microsponges includes two techniques: Liquid-liquid suspension polymerization and Quasi-emulsion solvent diffusion method. Their characterization and evaluation can be done in many ways like particle-size measurement and porosity, morphology, true density determination, analyzing the rheological properties, and dissolution studies. Present work focuses on the detailed study of the microsponge drug delivery system. This will help the reader to get all the information regarding the microsponge delivery systems.

Direct Compression Tablet Containing 99% Active Ingredient—A Tale of Spherical Crystallization

Direct compression (DC) is the easiest and most cost-effective process for tablet manufacturing, because it only involves blending and compression. However, active pharmaceutical ingredients generally exhibit poor mechanical and micromeritic properties, which necessitate dilution and the use of high percentage of excipients to enable a robust DC manufacturing process. Consequently, drug loading in DC tablets is usually low (typically <30%, w/w). In this study, spherical crystallization by the quasi-emulsion solvent diffusion method was used to engineer a poorly flowing model compound, ferulic acid (FA), to attain superior mechanical properties, particle size distribution, and morphology. The engineered FA particles enabled the successful development of DC tablets containing 99% FA, which is in sharp contrast to the maximum 10% FA loading using as-received FA. The record high active pharmaceutical ingredient loading in this work illustrates the potential for spherical crystallization to enable high drug loading when developing a tablet product using the DC manufacturing process.

Ocular administration of acetazolamide microsponges in situ gel formulations

In the present work, the antiglaucoma drug, acetazolamide, was formulated as microsponges in situ gel for ocular drug delivery aiming an improved therapeutic efficacy and reduction in the systemic side effects of oral acetazolamide. The microsponges were prepared by the quasi emulsion solvent diffusion method and were incorporated into 25% pluronic F-127 in situ gel. Ethyl cellulose polymer in different proportions with drug was used to prepare the microsponges. Different parameters were evaluated to select the best formulation. The formula S2 with drug to polymer ratio (2:1) showed high entrapment efficiency of about 82% and mean particle size of about 10 µm with polydispersity index (PDI) of 0.22, which are suitable characters for ocular delivery. The in situ gels were evaluated for physicochemical properties (pH, gelling capacity, gelation time and rheological properties) and in vivo studies. S2 formulation showed higher therapeutic efficacy compared to free drug in gel. It was non irritant to the rabbit's eye. These results indicated that acetazolamide microsponges in situ gel have potential ability for ophthalmic delivery.

Nanotechnological Approach to Increase the Antioxidant and Cytotoxic Efficacy of Crocin and Crocetin.

Crocin and crocetin are two interesting constituents of saffron (Crocus sativus) that possess important biological activities. Their use as therapeutic agents is strongly compromised by a scarce stability, poor absorption, and low bioavailability. Therefore, to improve these unfavorable features, the aim of the present work has been to apply a nanotechnological approach based on the formulation of solid lipid nanoparticles containing crocin and crocetin. Solid lipid nanoparticles were formulated according to crocin and crocetin chemical properties, using a variation of the quasi-emulsion solvent diffusion method to formulate crocin-solid lipid nanoparticles, while crocetin-solid lipid nanoparticles were prepared following the solvent diffusion method. Morphology and dimensional distribution of solid lipid nanoparticles have been characterized by differential scanning calorimetry and photon correlation spectroscopy, respectively, while the effect of drug incorporation versus time has been studied by Turbiscan technology. In order to verify the role of the nanotechnological approach on the biological activities of crocin and crocetin, the antioxidant and antiproliferative effects of these carotenoids once incorporated in lipid nanoparticles have been evaluated. For this aim, the oxygen radical absorbance capacity assay and the MTT test were used, respectively.The results pointed out the formulation of nanometric dispersions endowed with high homogeneity and stability, with an encapsulation efficiency ranging from 80 (crocetin-solid lipid nanoparticles) to 94% (crocin-crocetin). The oxygen radical absorbance capacity assay evidenced an interesting and prolonged antioxidant activity of crocin and crocetin once encapsulated in solid lipid nanoparticles, while the nanoencapsulation strategy showed a different mechanism in ameliorating the cytotoxic effect of these two substances.