Release Kinetic Studies Research Articles

Zinc micronutrient-loaded carboxymethyl tamarind kernel gum-based superabsorbent hydrogels: controlled release and kinetics studies for agricultural applications

The novel zinc-loaded superabsorbent hydrogel (ZSAH) was synthesized through in situ incorporation of zinc micronutrient in carboxymethyl tamarind kernel gum cross-linked network. The synthesized ZSAH was characterized by FTIR, SEM, TGA, swelling studies, etc. and found to have good water absorption capacity (410 g/g in distilled water) and with entanglement of zinc with weak physical forces. The ZSAH thus synthesized was assessed for controlled release application in soil as well as water, to test its application in the field of agriculture. The ZSAH exhibited slow and steady release pattern of zinc with 55% release within 72 h in water, and 83% release within 80 days in soil. Under the release kinetics studies, Korsmeyer-Peppas model was found to be best explaining the zinc release pattern through ZSAH. The ZSAH followed Fickian mechanism for release and it was observed that the diffusion was independent of the structure of the polymeric network. The time for zinc release from ZSAH, predicted as per the Olson’s single exponential model, revealed significantly prolonged T99 (time for release of 99% Zn) in water (12.22 days) as also in soil (625 days). Hence, the novel synthesized ZSAH exhibited great potential as a zinc micronutrient delivery system in agriculture.

Fabrication of Mupirocin-Loaded Nanostructured Lipid Carrier and Its In Vitro Characterization.

In the present study, mupirocin (MP), an antimicrobial agent, was formulated as a nanostructured lipid carrier (NLC) by using a novel method named as melt emulsion ultrafiltration method. For the formulation of NLC, glyceryl monostearate and watermelon seed oil were used as solid and liquid lipids, respectively. The method was optimized for various parameters by Taguchi design of experiment and prepared NLCs were characterized for particle size, polydispersity index (PDI), shape, zeta potential, % drug loading, and in vitro release profile. The optimized NLCs were found to be smooth, monodisperse with PDI 0.229 ± 0.093. NLCs were found to have an average particle size of 139 ± 0.75 nm and +21.9 ± 0.98 mV as zeta potential. The % drug loading of optimized NLCs was found to be 59% ± 0.13%. The optimized NLCs were able to release the drug up to 24 h. The release kinetic study revealed mixed-order kinetics. Hence, it was concluded that the novel method is simple and able to fabricate MP-loaded NLCs with sustained release property and being stable in terms of particle size, PDI, and % drug loading.

Clinoptilolite Microparticles as Carriers of Catechin-Rich Acacia catechu Extracts: Microencapsulation and In Vitro Release Study.

The main goal of the present study was to investigate the microencapsulation, in vitro release capacity and efficiency of catechin-rich Acacia catechu extract by Clinosorbent-5 (CLS-5) microparticles by in-depth detailed analyses and mathematical modelling of the encapsulation and in vitro release kinetics behaviour of the polyphenol-mineral composite system. The bioflavanol encapsulation and release efficiency on/from the mineral matrix were assessed by sorption experiments and interpretative modelling of the experimental data. The surface and spectral characteristics of the natural bioactive substance and the inorganic microcarrier were determined by Fourier Transform Infrared Spectroscopy (FTIR) and Ultraviolet/Visible (UV/Vis) spectrophotometric analyses. The maximum extent of catechin microencapsulation in acidic medium was 32%. The in vitro release kinetics study in simulated enzyme-free gastric medium (pH = 1.2) approved 88% maximum release efficiency achieved after 24 h. The in vitro release profile displayed that the developed bioflavanol/clinoptilolite microcarrier system provided sustained catechin in vitro release behaviour without an initial burst effect. Thus, the results from the present study are essential for the design and development of innovative catechin-CLS-5 microcarrier systems for application in human and veterinary medicine.

Metronidazole Loaded Polycaprolactone-Carbopol Blends Based Biodegradable Intrapocket Dental Film for Local Treatment of Periodontitis

Objective: The goal of this research was to optimize and evaluate an intrapocket dental film, composed of polycaprolactone and carbopol blends for the management of periodontitis. Methods: The intrapocket dental film was prepared using a modified solvent casting method, followed by characterization, in-vitro release, in-vitro antimicrobial activity, and in-vivo efficacy on the periodontitis animal model. Results: Prepared films were consistent in thickness (2.10±0.56 to 2.50±0.39 mm) and weight (35.23±0.37 to 39.45±0.45 mg) with drug entrapment of up to 87.63±1.98 percent. The concentration of carbopol is observed to have a direct relationship with the thickness, film weight, and swelling factor of the prepared dental film. The film has a surface pH close to gingival crevicular fluid pH and is therefore appropriate for the application. The developed film exhibited a biphasic drug release profile with an initial burst release followed by a continuous release for more than 11 days. Drug release kinetic study supports the release of the drug by a diffusion-based process, as best explained by the Korsmeyer Peppas kinetics (R2 =0.9635). in vitro antimicrobial activity was also in accordance with drug release, with a high initial zone of inhibition (ZOI) (49.32±0.156mm), followed by 14.28±0.080 mm ZOI on the 11th day. The in vivo study showed that the prepared film was able to prevent periodontal ligament degeneration, as observed in the periodontitis experiment animal model. Conclusion: The prepared intrapocket dental film based on caprolactone and carbopol can be used as a novel local drug delivery system for the management of periodontitis.

Controlled release and release kinetics studies of boron through the functional formulation of carboxymethyl tamarind kernel gum-based superabsorbent hydrogel

The novel Boron micronutrient-loaded superabsorbent hydrogel (BSH) was synthesized via in situ mechanism having carboxymethyl tamarind kernel gum (CMTKG) as its principle component. The synthesis was established by thermal gravimetric analysis examination, scanning electron microscopy micrographs studies, and Fourier transform infrared analysis. The influence of various solvents, such as standard saline solution, different pH solutions (4, 9, 12), and distilled water on the swelling degree of BSH, was examined. Out of all the mentioned solvents, the highest swelling degree was noticed by the distilled water (465 g/g). The BSH was also examined for the agricultural application to assess the release of the boron micronutrient. It was established by studying and calculating the release behavior pattern along with the release kinetics of BSH in water, and as well in soil. It is significant to note that in soil, BSH exhibited 20.07% for the 1st day which notably increased to 76.17% on the 80th day. Release kinetic studies suggested that the Korsmeyer–Peppas model fitted the best out of all the models used, in the case of water, which also revealed that the release of boron from BSH was independent of the polymeric network as it followed Fickian diffusion mechanism. However, in the case of soil, the release was observed to follow the Higuchi model. The half-life and time period for the release of 95% and 99% were calculated as per the Olson’s single exponential model, to predict the pattern of boron release from developed BSH formulation. Release time for 99% boron in the soil, 274 days (with a half-life of 38 days), was found higher than in water, 9.33 days (with a half-life of 1.29 days). Thus, moisture-retaining BSH also successfully revealed slow boron release behavior.

Development and Characterization of Drug‐Loaded PVP/PAN/Gr Electrospun Fibers for Drug Delivery Systems

AbstractThe objective of the present study is to evaluate the pH‐dependent drug release from polyvinylpyrrolidone (PVP)/polyacrylonitrile (PAN)/graphene (Gr) (P1) fibers using a quartz crystal microbalance (QCM). Electrospun fibers for poorly water‐soluble drugs were prepared on the QCM electrode surface through the electrospinning with P1 as the fiber‐forming polymer and drug carrier system and ibuprofen (Ibu) as the model drug. Characterization of the fibers is practiced by X‐ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy in combination with energy‐dispersive X‐ray spectroscopy (SEM‐EDX), thermogravimetric analysis (TGA)‐differential scanning calorimetry (DSC), and water contact angle measurements. The in vitro release kinetic studies of the Ibu were studied using QCM and UV‐vis spectroscopy. The drug delivery properties of the fibers of PVP/PAN/Gr with 5 wt % Ibu (P2) and PVP/PAN/Gr with 10 wt % Ibu (P3) were measured at pH 5.4 and 7.4. In pH 5.4, the cumulative drug release of 19.5 % was procured from the P3 fiber within 24 h, on the other hand; the cumulative drug release of 16 % was acquired in pH 7.4.

Release Kinetics Studies of Early-Stage Volatile Secondary Oxidation Products of Rapeseed Oil Emitted during the Deep-Frying Process.

The research concerns the use of proton transfer reaction mass spectrometer to track real-time emissions of volatile secondary oxidation products released from rapeseed oil as a result of deep-frying of potato cubes. Therefore, it was possible to observe a sudden increase of volatile organic compound (VOC) emissions caused by immersion of the food, accompanied by a sudden release of steam from a potato cube and a decrease of the oil temperature by more than 20 °C. It was possible to identify and monitor the emission of major secondary oxidation products such as saturated and unsaturated aldehydes, namely acrolein, pentanal, 2-hexenal, hexanal, 2-nonenal and 2-decenal. Each of them has an individual release characteristic. Moreover, the impact of different initial frying temperatures on release kinetics was investigated. Subsequently, it was possible to approximate the cumulative emission by a second-degree polynomial (R2 ≥ 0.994). Using the proposed solution made it possible for the first time to observe the impact of the immersion of food in vegetable oil on the early emission of thermal degradation products oil.

Extended release of 6-aminopenicillanic acid by silanol group functionalized vermiculite

The present study aimed to improve capability of vermiculite for extended release ofdrug such as: 6-Aminopenicillanic acid (6-APA). For this purpose, functionalization of vermiculite (VMT) was done by utilizing silanol through hydrolyzing of tetraethoxysilane. The synthesized samples characterized through the XRD, FTIR and BET analyses. The Maximum obtained 6-APA absorption capacity of VMT-Si was 243.9 mg/g, which was higher than other clays. The equilibrium studies demonstrate that drug absorption on VMT and VMT-Si is homogeneous and heterogeneous, respectively. Kinetic studies have been performed by applying reaction based models (such as: pseudo-first-order and pseudo-second-order) and diffusion based models (such as: Boyd, intra-particle diffusion and mass transfer models), which indicates the chemisorption interaction of both aforementioned compounds. The in-vitro release profile of VMT showed a release of about 52% after 5 hours. Whereas, the in-vitro release profile of 6-APA from VMT-Si showed substantially less release of 70% after 7 hours compare to VMT. The maximum obtained release amount of antibiotic (6-APA) per each gram of VMT-Si-6APA and VMT-6APA was 167 mg and 45 mg, respectively. Release kinetic studies show that the release mechanism of 6-APA is controlled by the diffusion process based on Fick's law. In conclusion, vermiculite functionalization with silanol, reduced the rate of drug release and increased the amount of released 6-APA.

Investigation of polyelectrolyte multilayers deposited on corona charged composite polylactic acid / poly(ε-caprolactone) substrates

In the present study chitosan and casein polyelectrolyte multilayers (PEMs) deposited on composite polylactic acid (PDLA) / poly(ε-caprolactone) (PEC) substrates were investigated. The substrate’s morphology was investigated using polarized light microscopy and their degree of crystallization was studied by the application of differential scanning calorimetry. The substrates obtained were charged in a corona discharge system, consisting of a corona electrode (needle), a grounded plate electrode, and a metal grid placed between them. Positive or negative 5 kV voltage was applied to the corona electrode. 1 kV voltage of the same polarity as that of the corona electrode was applied to the grid. The dependences of the normalized surface potentials on the storage times of positively and negatively charged substrates were studied. Layer-by-layer (LbL) technique was used for multilayer deposition on the substrates. PEMs with different number of layers (4 or 8) were obtained. A model drug Benzydamine hydrochloride was loaded in the casein layers in order to evaluate the effect of the kind of substrate on the drug immobilization and release. A study of the drug release kinetics in saline buffer was carried out and the amount of the released drug was calculated spectrophotometrically. It was shown that the experimental results fit to the Peppas model with a very good level of correlation and the model parameters differ depending on the used substrate.

Release, transfer and partition of fluorescent dyes from polymeric nanocarriers to serum proteins monitored by asymmetric flow field-flow fractionation

Fluorescent probes are used in drug nanocarrier pre-clinical studies or as active compounds in theranostics and photodynamic therapy. In the biological medium, nanoparticles interact with proteins, which can result in the off-target release of their cargo. The present study used asymmetric flow field-flow fractionation with online multi-angle laser light scattering and fluorescence detection (AF4-MALLS-FLD) to study the release, transfer, and partition of fluorescent dyes from polymeric nanoparticles (NP). NP formulations containing the dyes Rose Bengal, Rhodamine B, DiI, 3-(α-azidoacetyl)coumarin and its polymer conjugate, Nile Red, and IR780 and its polymer conjugate were prepared. NP suspensions were incubated in a medium with serum proteins and then analyzed by AF4. AF4 allowed efficient separation of proteins (< 10 nm) from fluorescently labeled NP (range of 54 – 180 nm in diameters). The AF4 analyses showed that some dyes, such as Rose Bengal, IR780, and Coumarin were transferred to a high extent (68-77%) from NP to proteins. By contrast, for DiI and dye-polymer conjugates, transfer occured to a lower extent. The studies of dye release kinetics showed that the transfer of IR780 from NP to proteins occurs at a high extent (~50%) and rate, while Nile Red was slowly released from the NP over time with reduced association with proteins (~20%). This experiment assesses the stability of fluorescence labeling of nanocarriers and probes the transfer of fluorescent dyes from NP to proteins, which is otherwise not accessible with commonly used techniques of separation, such as dialysis and ultrafiltration/centrifugation employed in drug encapsulation and release studies of nanocarriers. Determining the interaction and transfer of dyes to proteins is of utmost importance in the pre-clinical evaluation of drug nanocarriers for improved correlation between in vitro and in vivo studies.

Bursting the Virulence Traits of MDR Strain of Candida albicans Using Sodium Alginate-based Microspheres Containing Nystatin-loaded MgO/CuO Nanocomposites.

IntroductionCandida albicans is a major opportunistic pathogen that causes a wide range of human infections. Currently available therapeutic agents are limited for treating these fungal infections due to multidrug resistance as well as their nonbiodegradability, poor biocompatibility and toxicity. In order to battle these limitations, we have synthesized a polymeric system as microcarriers to deliver the antifungal drug. The objective of the present study was to immobilize MgO/CuO nanocomposite and nystatin-loaded MgO/CuO nanocomposites in nontoxic, nonimmunogenic, biodegradable and biocompatible sodium alginate microspheres for the first time.Materials and MethodsNanoparticle-loaded sodium alginate microspheres were prepared by ionotropic gelation technique using calcium chloride as a cross-linker. Synthesized microspheres were characterized using standard characterization techniques and were evaluated for biological activity against MDR strain of C. albicans.ResultsCharacterization of microspheres by Fourier-transform infrared spectroscopy confirmed loading of Nys-MgO/CuO NPs, scanning electron microscopy (SEM) revealed rough spherical beads with a highly porous surface having an average size in the range of 8–10 µm. X-ray diffraction (XRD) analyzed its semicrystalline structure. Entrapment efficiency of Nys-MgO/CuO NPs was 80% and release kinetic study revealed sustained and prolonged release of drug in pH 5.5. Flow cytometry analysis showed yeast cell death caused by Nys-MgO/CuO MS exhibits late apoptotic features. In cytotoxicity assay 5–14 mg of microspheres did not cause hemolysis. Microspheres reduced virulence traits of C. albicans such as germ tube and biofilm formation were compromised at concentration of 5 mg/mL. Antimicrobial assessment results revealed a pronounced inhibitory effect against C. albicans.ConclusionThe in vitro experiments have shown promising results based on good stability, Nys-MgO/CuO NP-encapsulated microspheres can be used as a prolonged controlled release system against MDR pathogenic C. albicans.

Formulation and evaluation of buccal bioadhesive tablets using glimepiride as a model drug

Objectives: The present investigation is concerned with formulation and evaluation of bioadhesive buccal tabletscontaining antidiabetic drug, Glimepiride to circumvent the first pass effect and to improve its bioavailability because bioadhesion has shown renewed interest for prolonging the residence time of bioadhesive dosage forms through various mucosal routes in drug delivery applications. Bioadhesive-based topical and local systems have shown enhanced bioavailability. Bioadhesive drug delivery gives rapid absorption and good bioavailability due to itsconsiderable surface area and high blood flow. Drug delivery across the mucosa bypasses the first-pass hepaticmetabolism and avoiding the degradation of gastrointestinal enzymes and with reduction in dosing frequency and dose related side effects. Methods: The tablets were prepared by direct compression method. Six formulations weredeveloped with varying concentrations of polymers like sodium alginate, PVP and magnesium stearate. The tabletswere tested for weight variation, hardness, surface pH, drug content uniformity, percentage swelling index,bioadhesive strength, ex-vivo residence time in-vitro drug dissolution study, in-vitro drug release kinetic study, exvivo permeation study and Stability study. Results: FTIR studies showed no evidence on interactions between drug, polymers, and excipients. The surface pH, bioadhesive strength was found to be 6.22, 16g and, respectively. The formulation containing 4 mg of Glimepiride exhibited 6 h sustained drug release i.e. 93.98±0.8% with desiredtherapeutic concentration. The drug permeation from the formulation was slow and steady and 3.56 mg of Glimepiride could permeate through sheep buccal membrane with a flux of 0.27 mg hr-1 cm-2. The in-vitro release kinetics studies reveal that the formulation fits well with zero order kinetics. Conclusion: Hence, it was concluded that the formulation was suitable for all the evaluation parameters and can be permeated through human buccal mucosa.

Electrospinning, Preparation and Characterization of Polyvinylidene Fluoride / Pectin Electrospun Loaded with Benzalkonium Chloride as a Drug Reservoirs

Porous nanofiber electrospun of polyvinylidene fluoride (PVDF)/pectin was successfully developed using electrospinning method containing benzalkonium chloride (BAC) as a drug model for the controlled drug delivery system assessment. The electrospun was tested for its mechanical, morphological, and wettability properties. Scanning electron microscope (SEM) micrograph demonstrated that the smooth surfaces of nanofibers morphology had achieved up to 2 wt% pectin inclusion with optimum fiber diameter, 143 ± 1.4 nm. The optimized scaffold PVDF/Pectin showed that the reduction of mechanical integrity and the optimum value of tensile strength, modulus strength, and elongation at break were 5.98 ± 0.17 MPa, 16.82 ± 0.10 MPa, and 79.3 ± 1.3% MPa. Water contact angle analysis and degree of swelling suggested that the inclusion of pectin had enhanced the wettability properties of hydrophobic PVDF electrospun with the highest swelling capacity achieved of 78.9 ± 1.7%. The in vitro drug release tests using BAC, which was released from the hybrid electrospun nanofibers, achieved prolonged release profile due to the elimination of the uncontrollable initial burst release. Kinetic release study from Higuchi Model and Korsmeyer-Peppas further validates that the drug release mechanism is only influenced by the diffusion factor. The present study indicates the potential of PVDF/pectin electrospun nanofibers to be exploited as a tool for a sustainable drug delivery system.

Preliminary Evaluation of an Autologous Dendritic Cell Vaccine Using Nanoparticle Technology for the Treatment of Canine Malignant Melanoma

Canine malignant melanoma is an aggressive neoplasm that carries a poor prognosis due to its minimal responsiveness to traditional therapy protocols, particularly if the oral cavity, mucocutaneous junctions, or subungual sites are involved. This proof-of-concept study evaluated a prototype autologous dendritic cell vaccine using poly-lactic-co-glycolic (PLGA) nanoparticles containing antigens from patient-derived whole tumor lysate and the adjuvant monophosphoryl lipid A in five canines with stages III-IV malignant melanoma. Nanoparticle constructs biochemical characterization; encapsulation efficiency and kinetic release studies were determined. Our results showed that tumor antigens were successfully incorporated in the PLGA/monophosphoryl lipid A nanoparticle constructs. Additional in vitro experiments showed that the PLGA/monophosphoryl lipid A nanoparticle constructs effectively activated autologous dendritic cells, and generated a greater than twofold increase in the release of the pro-immune cytokine IFN-γ. No significant adverse effects were observed in any of the patients following intradermal vaccination, and flow cytometry of whole blood revealed increased CD4:CD8 T lymphocyte ratios by the completion of the study. These results suggest that a dendritic cell vaccine utilizing PLGA/monophosphoryl lipid A nanoparticle technology could potentially initiate an adaptive immune response and is safe to administer to canine patients. Further in vivo studies with a larger cohort of patients are warranted.

Exploration of Inbuilt Novel Properties as Bioretardant Cum Stabilizer of Isolated Biopolymer from Fragaria ananassa in Delivery of Nanosized Phenytoin.

The research aims to develop bionanosuspension using a biopolymer isolated from Fragaria ananassa fruit that constitutes potential and natural polymeric properties. At first, the biomaterial was isolated from the natural fruit pulp of Fragaria ananassa by an economical method of isolation. The model drug was nanosized by a novel sonication method. The isolated biopolymer was characterized for its polymeric properties, and its potential capabilities were evaluated in the delivery of nanosized phenytoin. The isolated biopolymer was characterized for DSC, FTIR, NMR, mass, and scanning electron microscopy. The isolated biomaterial was used for the preparation of phenytoin-loaded bionanosuspension with other excipients. The bionanoparticles were also characterized by different analytical testing such as FTIR, DSC, and SEM to confirm any interaction between model drug and biopolymer.The prepared bionanoparticles showed the release of phenytoin in a sustained manner over 36 hours. The release kinetic study was done using the BIT-SOFT 1.12 software and other parameters such as t50%, t80%, and r2 were calculated. The formulation PFr6 was considered best having t50% in 18.22 hours and t80% in 29.62 h with an r2 value of 0.9793. This formulation showed up to 87.89% drug release within 36 hours. The prepared bio-nanosuspension was found to be stable and in a well-dispersed state. The dried bionanosuspension evaluation revealed no interaction between model drug and biopolymer without any loss of characteristic peaks. Therefore, the isolated biopolymer can be safely used to prepare stable bionanosuspension loaded with nanosized phenytoin.

Formulation and In Vitro Evaluation of Tropisetron Loaded Microspheres

Tropisetron is a 5-HT3(5-hydroxytryptamine3) receptor antagonist used fortheprevention of chemotherapy-induced nausea and vomiting. In the present study, ethyl-cellulose, sodium alginate and HPMC K15M loaded microspheres of tropisetron were successfully prepared by ionic gelation technique. All the formulations were evaluated forvarious parameters such as drug content, entrapment efficiency, in vitrodissolution study, release kinetic study and stability study. The in vitro dissolution studies showed that tropisetron microspheres formulation F10 havebetter sustained effect over a period of 12 hours which contains all three polymers having a perfect controlled release. The mechanism of release was determined byvarious kinetic equations such as zero-order, first-order, Higuchi, Hixon Crowell, Korsmeyer-Peppas and finding the R2values of the release profile corresponding to each model. Thus, in thepresent study,in vitro drug release kinetic of the best formulation followed zero order release kinetic model and the drug release mechanism was anomalous diffusion. The results of the current study clearly indicate a promising potentialdelivery systemof the tropisetron microsphere as an alternative to the conventional dosage form

Fabrication of drug-loaded ultrafine polymer fibers via solution blowing and their drug release kinetics

Biocompatible polymer fibers have garnered significant interest due to their unique properties. Applications range from absorbent media to tissue engineering and drug delivery products. Many manufacturing processes produce such fibers, but a gap exists in highly scalable processes for fibers loaded with thermolabile additives like pharmaceuticals. This study investigates preliminary process-structure-function relationships of solution blown poly(ethylene oxide) fibers loaded with doxycycline, a drug that has demonstrated antibiotic, anti-inflammatory, and anti-tumoral properties. After parameter screening, a factorial experiment mapped the solution blowing design space with a multi-nozzle apparatus. A 1 mm-thick mat was fabricated comprising doxycycline loaded polymer fibers with a mean diameter of 552 ± 200 nm. Study of release kinetics showed the doxycycline released with a significant burst effect over approximately 1 minute. This study highlights solution blowing as a scalable manufacturing platform for fabricating poly(ethylene oxide) fibers loaded with this impactful drug.

Development of Sustained Release Eudragit Based Matrix Tablet of Fluvastatin Sodium Microspheres

The purpose of this research is to investigate the suitability of acquiring improved dissolution profile and sustained release of Fluvastatin sodium to reduce dosage frequency via a novel combination of freeze dried microspheres and Eudragit polymers-based matrix tablet technologies. Fluvastatin sodium microspheres were prepared using polyvinyl pyrollidone K-30 and Poloxamer 407 through solvent evaporation via freeze drying. We adopted a central composite design to examine the influence of independent variables viz. drug:polymer (X1) and surfactant (X2) on the t50 % (Y1), Q90 (Y2) and percentage drug content (Y3) along with determination of an optimized composition for production of an optimal Fluvastatin sodium microspheres. Design expert software illustrated that an optimized Fluvastatin sodium microspherescould be achieved using 1:3.496 drug:polymer and 3.102 % poloxamer 407 which would illustrates t50 % (36.33 min), Q90 (79.99 %) and percentage drug content (81.589 %). The mean diameter and polydispersity index of Fluvastatin sodium microspheres using dynamic light scattering was found 0.78 μm and 0.287, respectively. Sustained release tablet of optimized Fluvastatin sodium microspheres (Fluvastatin sodium microspheres-sustained release tablet) was manufactured using Eudragit RS 100 and Eudragit RL 100 based granules by wet granulation technique. In vitro drug release kinetics studies were executed to assess the drug release mechanism from optimized Fluvastatin sodium microspheres and Fluvastatin sodium microspheres-sustained release tablet. The dissolution level of Fluvastatin sodium was 3.58-fold improved wthin 2 h through the freeze dried microspheres. Fluvastatin sodium microspheres-sustained release tablet showed sustained drug release over 24 h and was matched properly to Korsmeyer-Peppas model with release exponent of 0.5318, which indicated drug release through diffusion and erosion mechanism. Conclusively, it has been demonstrated that novel combination of freeze dried microspheres and their Eudragit polymers-based matrix tablet techniques could find great potential for improving drug dissolution and sustained release of water insoluble drugs along with reduced dosage frequency.

Development of Donepezil Hydrochloride Loaded Gellan Gum Based Nasal Mucoadhesive Microspheres by Spray Drying Method

Abstract: Objectives: The aim of present study was the formulation of donepezil hydrochloride loaded polymeric mucoadhesive microspheres for delivery via nasal route to increase the residence time and absorption of drug from the nasal mucosa. Methodologies: The microspheres were formulated by conventional spray drying technique by using gellan gum as a mucoadhesive polymer. A 32 full factorial design was utilized with polymer concentration (X1) and liquid feed flow rate (X2) as independent variables in formulation of the microspheres and their effect was studied on entrapment efficiency, particle size and drug loading. Results: The results specified that the X1X2 interaction had significant effect on drug loading while X2 alone effect on entrapment efficiency and particle size. The optimized microspheres were further evaluated for drug release kinetic study, histological examination, ex vivo permeation study and stability study. Conclusion: It was concluded that the gellan gum containing microspheres of donepezil hydrochloride with mucoadhesive property are suitable for nasal delivery. Key words: Mucoadhesion, Intranasal, Microsphere, Donepezil hydrochloride, Spray drying.

Design and release kinetics of liposomes containing abiraterone acetate for treatment of prostate cancer

The present work deals with the preparation and in vitro evaluation of liposomal formulations of abiraterone acetate. In the present work, abiraterone acetate-loaded liposomal formulation was formulated by thin lipid film method. The prepared liposomal formulation of abiraterone acetate was evaluated by drug content estimation, particle size measurement, in vitro drug release and release kinetics studies. Dried samples of liposomal suspension of abiraterone acetate were characterized by scanning electron microscopy (SEM) analysis. The drug contents of liposomal formulations were within the ranges, 6.06 ± 0.43 to 10.55 ± 1.04 mg/ml. In vitro drug release from these liposomal formulations was found to be sustained over 4 h, which followed the zero order model (R2 = 0.8940 to 0.9884) over 4 h. After storage of 1 month at 4 °C temperature, the best liposomal formulation (prepared using 100 mg lecithin) was found stable enough. These liposomal formulations of abiraterone acetate can be formulated for parenteral application to treat advanced prostate cancer.