oleic acid (OA), MNPs were coated with OA (MNPs-OA) before moving to the toluene phase with the addition of salt. At OA concentration of 0.3 wt%, most of the nucleated MNPs were hydrophobic and well dispersed in the toluene phase. Using DVB as a monomer for ms CRP, high encapsulationefficiency (92 %EE) of MNPs-OA was obtained, with low free polymer particle formation. By contrast, large amounts of free polymer particles were observed at low %EE (32%) of MNPs. The main driving force for high %EE was obtained by coating the surface of the MNPs by OA which increased hydrophobicity.
LPD as an effective nanovector for systemic siRNA delivery has high encapsulationefficiency, not only because of the positive charge, but because of the thymus DNA used as a carrier in this formulation to improve core compaction. The different Fab’ conjugation technologies used for LPD did not change the particle structure (Figure 3), but the effect on encapsulationefficiency remains unknown. It was found that the siRNA encapsulationefficiency of all liposomes was as high (about 90%) as that of naked LPD (Figure 4B), which is consistent with the result obtained from the gel retardation assay, indicating that there was hardly any impact on siRNA
Acyclovir (ACV), analog of 2′-deoxyguanosine, is known for its antiviral activity against Herpes simplex virus (HSV). A major limitation of treatment with acyclovir is high distribution and low half-life that leads to taking high doses of acyclovir. Recent studies have shown that entrapment of acyclovir in nano-carriers can increase effectiveness and also decrease side effects of the drug. Therefore, in the present study the preparation and characterization of acyclovir loaded nano- niosomes was investigated. The non-ionic surfactant vesicles were prepared by thin film hydration method. The lipid composition in optimal formulation consisted of Span, cholesterol and D-- tocopheryl polyethylene glycol succinate (TPGS) in the molar ratio of 55 : 30 : 15, respectively. Physical characteristics of optimized niosomes such as particle size, encapsulationefficiency (EE) and in vitro drug release were evaluated. Furthermore, the in vitro cytotoxicity study of empty niosomes (E-N), acyclovir loaded niosomes (ACV-N) and ACV as a free drug against Hela cell line was performed by MTT assay. The average of particle size and EE for optimized niosomes were 122.6 ± 0.2 nm and 24 % respectively. The drug release profiles proved the efficacy of optimized niosomes in prolonged release of ACV, so that the percent drug release for 1h was recorded as approximately 11.7 %. The prepared niosomes also showed significant stability with regard to particle size and EE when stored at least for seven days at 5˚C. The results of this study revealed ACV-N (F5) have a higher antiviral activity compared with free drug, and could be a suitable carrier for delivery of acyclovir in the treatment of HSV-1 infections.
different chemotherapy regimens, the drug has poor biological half life after intravenous injection(20). Moreover, the potent anti-cancer drug has exhibited toxicity in different organs and systems such as gastrointestinal, dermatological and central nervous system(19). Therefore, many researchers have proposed the encapsulation of MTX in different carriers (21-23). Among them, PLGA has exhibited better physiochemical properties such as high encapsulationefficiency and drug release(23).
The drug loading and encapsulationefficiency of fabricated nanoparticles is shown in Table 2. It was observed that with increase in the concentration of sodium alginate, encapsulationefficiency and drug loading were also found to increase, owing to increase in viscosity of the aqueous medium. But the encapsulation efficacy increased with increasing in calcium chloride concentration. When quantity of calcium chloride was increased, it promoted the solubilisation of drug in the aqueous phase.
It concluded that method of preparation of transformation type liquid crystals is simple and does not require any specific equipment. Encapsulationefficiency is also higher and viscosity of all the formulation found in the acceptable range. In vitro release profile of the drug offered controlled release of drug that can be utilized for once in a day application. Therefore, on the basis of method of preparation and evaluation, further it can be concluded that formulation may be simple, economic and easy to apply for once a day application in the management of mild to moderate hypertension.
The purpose of this work is to evaluate the possibility of enzyme therapy through microencapsulation of serratiopeptidase (SP) in biodegradable nanoparticles of chitosan (CS). This drug has short biological half life and thus frequent administration makes it a suitable candidate for controlled release. In this study, serratiopeptidase loaded chitosan nanoparticles were prepared by ionotropic gelation of CS with tripolyphosphate (TPP) anions. Reversible physical cross-linking by electrostatic interaction, instead of chemical cross-linking, has been applied to avoid the possible toxicity of reagents and other undesirable effects. The enzyme loaded particles optimized formulation was coated with sodium alginate solution to protect its release in stomach. The enzyme loaded nanoparticle formulations were characterized for morphology, particle size, encapsulationefficiency and in-vitro drug release. The preliminary studies show that TPP and CS were compatiable with SP. The ratio of CS to TPP has an influence on the mean particle size and when CS: TPP is 4:1 nanoparticles with smallest diameter are formed. Entrapment efficiency depends on the degree of deacetylation of chitosan. The formulation F-3 showed 96.7 % in-vitro drug release at 24 hours in PBS at pH7.4 and only 22.03% at 2 hr in SGF at pH 1.2. It is inferred that dissociation of the associated macromolecule from chitosan predominantly governs the release process. This dissociation is in turn, affected by the intensity of the interactions and the ionic strength of the release medium.
In the process of preparation of chlorothalonil microcapsules, factors of affecting particle size and encapsulationefficiency include shear speed, shear time, stirring speed, stirring time, the material and amount of solvent, and ratio of raw materials. Most of them were determined by a series of pre-experiments. The results were that optimal shear speed was 2500r/s, optimal shear time was 16min, optimal stirring speed was 1500r/s, and optimal stirring time was 30min. The most important factor, ratio of raw materials, was determined by following orthogonal experiments.
5. Method Development for Preparation of Voriconazole loaded Liposomal suspension The micro encapsulation vesicle (MCV) method is a liposome preparation technique that reproducibly produces liposomes with homogeneous particle sizes with high encapsulationefficiency. Liposomes encapsulating water-soluble drugs, lipophilic drugs and an amphiphilic drug were prepared by the MCV method and the encapsulationefficiency of the drugs was examined. 
Urea is a most widely used fertilizer in agriculture due to high nitrogen content, low cost, and commercial availability, but there are some finites related with in-effective used of the fertilizer, and environmental pollution. This study aim was to produce urea slow-release microcapsules using polycaprolactone as coating material by solvent evaporation method. The ratio of urea-PCL were 1:1, 1:2, and 1:3. Microcapsules obtained were characterized by Fourier Transform Infra-Red (FTIR), Scanning Electron Microscopy (SEM), particle size distribution, amount of urea entrapped in microcapsules, and release kinetics profile. There was no chemical interaction between urea and polycaprolactone. The result of SEM showed that microcapsules were spheric in shape with the rough surface and aggregate formed. Particle size distribution of coated urea microcapsules was in the range of 20-240 μm, influenced by the concentration of PCL. Encapsulationefficiency of urea microcapsules in formula 1, 2, and 3 were 80.28 ± 0.81, 82.65 ± 1.22, and 79.64 ± 0.65%, respectively. The percentage of release efficiency from formula 1, 2, and 3 were 58.85 ± 1.72, 26.76 ± 0.76, and 40.42 ± 2.39%, respectively. In conclusion, PCL could be used in microencapsulation formulation of urea slow release. The release kinetics of urea from microcapsules followed Langenbucher equation related with diffusion and erosion mechanism. PCl affected the release efficiency significantly (p<0.05).
To measure the 5-FU loading using high-performance liquid chromatography (HPLC), 5 mg dried 5-FU-loaded nanoHKUST-1 was treated with ultrasonic waves for 30 min with ethanol as an extraction reagent. We used a Dimma ODS-C 18 (200 × 4.6 mm, 5 µ m) column under the following conditions: mobile phase, methanol:water (20:80); flow rate, 1 mL/min; column temperature, 30 ° C; and injective volume, 10 µ L. An ultraviolet detector was used at a wavelength of 266 nm. Then, the 5-FU encapsulationefficiency was calculated as the percentage of drug that was effectively entrapped inside the NPs compared to the total drug used in the preparation procedure.
The core materials selected for zein encapsulations are generally hydrophobic or amphiphilic. This is related to the intrinsic tendency of zein to aggregate around these materials during EISA. The formation of self- assembled spheres could be subsequently triggered after the aggregation of zein around the core materials. However, this process is less applicable for highly hydrophilic substance, such as heparin , 5-fluorouraci , and pDNA . In spite of some reported experiments about the direct preparations of the above non-hydrophobic encapsulated zein micro/ nanoparticles, the morphology of the products was not satisfactory, which inevitably affected the encapsulationefficiency and drug delivery. Moreover, in these studies of micro/nano encapsulation, coacervation method is widely adopted to access smaller size. The micro/nanoparticles are obtained by desolvation of zein through the sudden addition of an aqueous solution while vigorous homogenizing or stirring is performed. However, the disadvantage has been pointed out that it may cause the loss of labile encapsulated ingredients in such high-energy method .
Table 1 lists composition of prepared formulations, en- capsulation efficiency and mean particle size of the hy- brid microspheres. It can be seen that the encapsulationefficiency of the hybrid microspheres for DS is always higher than 98%. This may be mainly attributed to elec- trostatic interaction between the microsphere carriers and the DS drug. In order to prove the electrostatic interac- tion, the zeta potentials of the hybrid microspheres and DS drug were determined at various pHs and are showed in Figure 1. It is shown that the isoelectric points of crosslinked CTS, CTS/APT-1 and CTS/APT-2 micro- spheres are pHs 8.14, 9.18 and 8.28, respectively; while the isoelectric point of DS is pH 4.03. This indicates that the hybrid microspheres show positive charge, and DS possesses negative charge in distilled water (pH 6.85). Therefore, a strong electrostatic interaction between the hybrid microspheres and DS leads to the higher encapsu- lation efficiency of the hybrid microspheres for DS.
In emulsion gelation method batches E1 to E6 showed %swelling in pH 1.2 and pH 7.4 ranges from 306.39 to 460.38 and 541.40 to 718.56 respectively. All Batches showed low swelling in pH 1.2 than phosphate buffer pH 7.4. At acidic pH, alginate is protonated into insoluble form of the alginic acid this displays low swelling and in intestinal pH, at pH 7.4 carboxyl groups of alginate ionize, which weakens the electrostatic interactions, thus making the bead structure loose resulting in increased swelling. Percent drug encapsulationefficiency for batches (E1- E6) ranges from 45.78% to 82.60%. The higher encapsulationefficiency was observed as the concentration of alginate increased. This is due to the greater availability of active calcium binding sites in
In order to promote a more efficient coacervation, the temperature, homogenization speed and morphology variables were evaluated. The study was conducted using samples obtained at different core concentrations (5, 7.5 and 10 g ·mL −1 ), since the formulations offer a greater separation into phases, determined by greater sediment mass and a less turbid supernatant. The formation of a large amount of coacervated mass does not necessarily mean that the oil was encapsulated, and it is necessary to evaluate the encapsulationefficiency.
The in vitro release study was performed using fabricated diffusion cell of formulation T1, T2 and T3. Study was performed for eight hours and samples were withdrawn in one hour interval. All three formulations showed controlled release property. Formulation T1 showed 79.33 % drug release in eight hour and formulation T3 showed 99.23 %. The r 2 value of in vitro release data were determined to find best fit model for different model like Zero order, First order, Higuchi Matrix and Peppas-Korsmeyer . All formulations showed zero order release profile, however formulation T1 shown more prominent. T1 formulation has good consistency on the basis of viscosity data, higher encapsulationefficiency and good crystalline property. All these parameters make T1 formulation as developed formulation.
Cilinidipine is a fourth generation N and L-type calcium channel antagonists used alone or in combination with another drug to treat hypertension. Cilnidipine is poorly water -soluble, BCS class II drug with 6 to 30 percent oral bioavailability due to first pass metabolism. So to protect the drug from degradation and improve its dissolution, solid lipid nanoparticles were prepared. Glyceryl monostearate was selected as lipid while span 20: tween 20 were selected as surfactant blends. The formulations were evaluated for various parameters, as percent transmittance, drug content, percent encapsulationefficiency; percent drug loading, In vitro drug release and particle size. Optimized formulation was lyophilized using lactose as a cryo-protectant. The lyophilized formulation was evaluated for micromeritic properties, particle size and in vitro dissolution. It was further evaluated for DSC, XRD, and SEM. Percent encapsulationefficiency and percent drug loading of optimized formulation (F3) were 78.66percent and 9.44percent respectively. The particle size of F3 formulation without drug was 204 nm and with the drug was 214 nm. The particle size of the reconstituted SLN was 219 nm. In DSC study, no obvious peaks for cilnidipine were found in the SLN of cilnidipine indicated that the cilnidipine must be present in a molecularly dissolved state in SLN. In X-ray diffractometry absence of peaks representing crystals of cilnidipine in SLN indicated that the drug was in an amorphous or disordered crystalline phase in the lipid matrix. Thus, solid lipid nanoparticle formulation is a promising way to enhance the dissolution rate of cilnidipine.
The increase in size of liposomes upon incorporation of cholesterol may have contributed to the observed increase of encapsulationefficiency and loading capacity of liposomes with increasing cholesterol content. Since the methanol extract of S. castaneifolia is highly soluble in hot water, it is expected to reside mainly in the aqueous interior of liposomes. Therefore, an increase in the size of liposomes may correspond to an increase in the encapsulationefficiency and loading capacity. Interestingly, our results are consistent with the results of Cagdas and coworkers demonstrating that incorporation of cholesterol in the lipid bilayer is essential for successful encapsulation of water soluble species in liposomes. The results of this study indicate that the encapsulation of water-soluble plant material may be increased by incorporating cholesterol in the lipid bilayer of phosphatidylcholine liposomes.
The encapsulationefficiency is related to the physio-chemical characteristic of both the core and wall material. Encapsulation efficiencies refer to the potential of the wall material to encapsulate or hold the core material inside the microcapsule. Encapsulation efficiencies are also related to the shelf life of the pigment content in the powder (Idham et al., 2012). The encapsulationefficiency of the spray dried encapsulated beetroot extract powder at varying temperature was found to be in the range of 96.79 to 99.60 for different ratio of wall to core material concentration 1:2, 1:4 and 1:6 as shown in Fig.3.1.Encapsulationefficiency increased with increasing inlet air temperatures for 1:2 and 1:4 core to wall material concentration at 120°C, 140°C, 160°C. It also depends on the surface betanin content if decreases in surface betanin content more it encapsulationefficiency. Surface betanin content is more in 1:2 (120°C) so that encapsulationefficiency is less. Similar result is reported by Anandaraman and Reineccius, 1986 for the encapsulated orange peel oil. Nunes and Mercadante, 2007 reported that the lycopene encapsulation using spray dryer (Lab plant SD-04, UK) with gum arabic and sucrose (8:2) with inlet and outlet temperatures of 170±2 and 113±2ºC respectively the microencapsulation efficiency ranged from 94 to 96%. The maximum efficiency of 86% was obtained for bixin encapsulated with gum arabic/sucrose (95:5),whereas with maltodextrin 20 DE this value was 54%, increasing to 75% with addition of an emulsifier to maltodextrin (Barbosa et al., 2005). In conclusion, since the efficiency found in the present work was higher than those obtained in the literature, combination of gum arabic and maltodextrin as wall material could be considered an excellent choice for the encapsulation of beetroot extract using spray drying technology.
ABSTRACT: In the recent days targeted drug delivery has gained more prominence for various advantages like site specific delivery and controlled release from the formulations. Amongst the plethora of avenues explored for targeted drug delivery, bioadhesive nanoparticles backed foremost attention offering local drug delivery and controlled drug release solving problems like tissue damage and drug wastage. Formulating nanoparticles with mucoadhesive polymers may provide a significant increase in the gastrointestinal residence time. Neostigmine bromide is a cholinesterase inhibitor used for the treatment of Myasthenia Gravis and is given by conventional routes like oral and intra venous. Bioadhesive nanoparticles of Neostigmine Bromide using synthetic and semi synthetic polymers like Carbopol, HPMC and ethyl cellulose were prepared by emulsification solvent evaporation method. The nanoparticles were characterized for their preformulation and post formulation parameters like compatibility, particle size, zeta potential, encapsulationefficiency, surface morphology, in vitro mucoadhesion, in vivo bioavailability, drug release and stability studies. Out of six, formulations F 1 and F 4 showed the best