Formulation of enteric coated microspheres containing pantoprazole

Pantoprazole is a first-line proton pump inhibitor drug for the treatment of gastric acid secretion disorders that is known to have minimal side effects and drug interactions. To improve its stability in gastric acid, delayed-release microspheres containing pantoprazole was prepared by emulsification-solvent evaporation using a polymer-containing mixture of hydroxypropyl cellulose (HPC) and ethyl cellulose (EC), which was then coated by alginate and EudragitL100. The morphological characteristics of the microspheres were examined by SEM, the particle size distribution inferred by laser diffraction, and the physical state of drug substance was measured by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and in vitro drug release. The three formulations of microspheres chosen for this study had an average size of 100 μm. The dissolution profile showed less than 10% of the drug was released after 120 min in 0.1-M HCl and more than 75% of drug was released after 45 min in a phosphate buffer with a pH of 6.8.

Formulation and Evaluation of Miconazole Nitrate Loaded Novel Nanoparticle Gel for Topical Delivery

The aim of the present research work is to design miconazole-loaded chitosan nanoparticles that could potentially assemble in wrinkle and hair follicles to provide prolong release to the skin tissue. The amount of drugs required for the preparation of nanoparticles was determined by studying the entrapment efficiency of preliminary batches. The emulsification/Solvent evaporation method was used for the preparation of nanoparticles. Different proportions of Miconazole Nitrate and Chitosan were dissolved in DCM. The size of the globules in the emulsion was reduced by a high energy shearing using a probe Sonicator at 50 % amplitude for 10 Minutes, followed by the addition of 10 ml 2% PVA. After overnight evaporation of DCM, for isolation of dried NPs, the NPs dispersion was centrifuged at 15,000 RCF for 30 minutes. The obtained particles were dispersed in de-ionized water and freeze-dried. 32 full factorial design was selected for optimization purposes. Prepared batches were evaluated for various parameters such as entrapment efficiency, production yield, particle size, zeta potential, and SEM. F5 batch was found to be optimized which was then used for the preparation of gel. Three levels of Carbopol934 and propylene glycol were used for the optimization of gel. The prepared gel was also evaluated for pH, drug content, viscosity, and spreadability. From the study, it was concluded that nanoparticle gel can be used for the treatment of various skin infections over the conventional gel.

Enhanced oral bioavailability and gastroprotective effect of ibuprofen through mixed polymer–lipid nanoparticles

Objectives: The aim of this study was to design and formulate mixed polymer–lipid nanoparticles (PLNs) for the delivery of ibuprofen. Methods: The mixed PLNs were prepared by a single modified emulsification solvent evaporation method. Key findings: Core-shell-shaped mixed PLNs were successfully prepared, with sizes in the nano range (193.3 ± 0.70 to 795.8 ± 0.70 nm) and ζ potential (−26.8 ± 0.45 to −42.8 ± 0.30 mV). Entrapment efficiency ranged from 80.3 to 93.6%. Conclusions: Pharmacokinetic parameters showed great improvement in Cmax and Tmax of ibuprofen from the formulation PLNs8 compared with the respective Brufen® and pure drugs, indicating improvement in bioavailability of the drug.

PLGA Based Nanospheres as a Potent Macrophage-Specific Drug Delivery System

Macrophages possess an innate ability to scavenge heterogenous objects from the systemic circulation and to regulate inflammatory diseases in various organs via cytokine production. That makes them attractive targets for nanomedicine-based therapeutic approaches to inflammatory diseases. In the present study, we have prepared several different poly(lactic-co-glycolic acid) (PLGA) polymer nanospheres for macrophage-targeted drug delivery using both nanoprecipitation and emulsification solvent evaporation methods. Two experimental linear PLGA polymers with relatively low molar weight, one experimental branched PLGA with unique star-like molecular architecture, and a commercially available PLGA, were used for nanosphere formulation and compared to their macrophage uptake capacity. The nanosphere formulations labelled with loaded fluorescent dye Rhodamine B were further tested in mouse bone marrow-derived macrophages and in hepatocyte cell lines AML-12, HepG2. We found that nanospheres larger than 100 nm prepared using nanoprecipitation significantly enhanced distribution of fluorescent dye selectively into macrophages. No effects of nanospheres on cellular viability were observed. Additionally, no significant proinflammatory effect after macrophage exposure to nanospheres was detected as assessed by a determination of proinflammatory cytokines Il-1β and Tnfα mRNA. All experimental PLGA nanoformulations surpassed the nanospheres obtained with the commercially available polymer taken as a control in their capacity as macrophage-specific carriers.

Preparation And Characterization Of 5-Fluorouracil Loaded Nanogels For Skin Cancer Treatments: In Vitro Drug Release, Cytotoxicity And Cellular Uptake Analysis

Objective: The present study aimed to explore the in-vitro anticancer potential of 5-fluorouracil (5-FU) loaded PLGA nanogels coated with nerolidol sesquiterpene. Methods: The emulsification-solvent evaporation technique was used for the preparation of plain PLGA nanogels (PNGs) and 5-FU loaded PLGA nanogels (FPNGs). A surface coating of Nerolidol (2%) sesquiterpene was employed to improve the penetration efficacy of the nanogels into stratum corneum. Results: The nanogels formulation FPNGs have the size range 220±0.25% nm obtained by dynamic light scattering. The entrapment efficiency approx ~ 42% with sustained release pattern for 24h estimated at different pH range. The cell uptake study and localization profile were revealed by confocal microscopy analysis using the HaCaT cell line. MTT assay demonstrated the cell compatibility of nanogels and confirms by apoptosis assay depicting the apoptotic index of 0.87. Conclusion: The carried study has concluded that FPNGs is a promising nanogels system against skin cancer that can be used to boost the chemotherapeutic efficiency of bioactive with sustained and controlled release at the desired site.

Nanosuspension as Promising and Potential Drug Delivery: A Review

In the last decade, nanosuspensions have gained considerable interest as a method for formulating poorly soluble drugs. Because of their cost-effectiveness and technological simplicity compared to liposomes and other colloidal drug carriers, nanoscale systems have recently received a lot of attention as a way of solving problems of solubility. Nanosuspensions are biphasic systems comprising of pure drug particles dispersed in an aqueous vehicle, stabilized by surface active agents. Fabrication of nanosuspension is simple and more advantageous than other approaches. Nanosuspension is a very finely single solid drug particle in an aqueous vessel, stabilized by surfactants for either oral or topical use or for parenteral and pulmonary administration, it can also be used for targeted drug delivery when incorporated in the ocular inserts and mucoadhesive hydrogels, with reduced particle size resulting in increased dissolution rate. This article covers the preparation of nanosuspension by bottom up technology, top down technology, melt emulsification, emulsification- solvent evaporation and supercritical fluid with their advantages and disadvantages, aspects of structure, classification and their drug delivery applications. Nanosuspension can be processed for the drugs which are of hydrophobic in nature quite easily employing stability enhancers, solvents that are of organic and additional ingredients including buffering agents, salts, PEG, osmotic agents and anti-freeze compounds.

Effect of Dexamethasone-Loaded PLGA Nanoparticles on Oral Mucositis Induced by 5-Fluorouracil

Oral mucositis (OM) is characterized by the presence of severe ulcers in the oral region that affects patients treated with chemotherapy. It occurs in almost all patients who receive radiotherapy of the head and neck, as well as patients who undergo hematopoietic cell transplantation. The pathophysiology of OM is complex, and there is no effective therapy. The aim of this study was to evaluate the effect of dexamethasone-loaded poly(d,l-Lactic-co-glycolic) nanoparticles (PLGA-DEX NPs) on an OM model induced in hamsters. The NPs were synthesized using the emulsification-solvent evaporation method and were characterized by the size, zeta potential, encapsulation efficiency, atomic force microscopy, physicochemical stability, and the in vitro release. The OM was induced by the administration of 5-FU on the first and second days and mechanical trauma on the 4th day of the experiment. PLGA-DEX NPs were administered to treat OM. The animals were euthanized on the 10th day. Macroscopic and histopathological analyses were performed, measurement of malonaldehyde (MDA) and ELISA was used to determine the levels of IL-1β and TNF-α. Immunoexpressions of NF-κB, COX-2, and TGF-β were determined by immunohistochemistry, and qRT-PCR was used to quantify the gene expression of the GILZ, MKP1, and NF-κB p65. The PLGA-DEX NPs (0.1 mg/kg) significantly reduced macroscopic and histopathological scores, decreased MDA, TNF-α and IL-1β levels, immunostaining for NF-κB, COX-2, TGF-β, and suppressed NF-κB p65 mRNA expression, but increased GILZ and MKP1 expression.

A review on designing Poly (lactic-co-glycolic acid) nanoparticles as drug delivery systems

: Poly (lactic-co-glycolic acid) (PLGA) is one of the versatile synthetic polymer comprehensively used in the pharmaceutical sectorbecause of its biocompatibility and biodegradability.These benefits lead to its application in the area of nanoparticles (NPs) for the drug delivery over the thirty years. This article offers to climb a general study of the different poly (lactic-co-glycolic acid) nanoparticles (PNPs) preparation methods such as emulsification-solvent evaporation, coacervation, emulsification solvent diffusion, dialysis, emulsification reverse salting out, spray drying nanoprecipitation, and supercritical fluid technology, from the methodological point of view.The physicochemical behavior of PNPs including morphology, drug loading, particle size and its distribution, surface charge, drug release, stability as well as cytotoxicity study and cellular uptake are briefly discussed. This survey additionally coordinates to bring a layout of the significant uses of PNPs in different drug delivery system over the three decades. At last, surface modifications of PNPs and PLGA nanocomplexes (NCs) are additionally examined.

Preparation of Temozolomide Nano SustainedRelease Microsphere Material and Its Application in Treatment of Glioma

The polylactic acid/glycolic acid (PLGA) sustained-release microspheres are used as the main material for local sustained-release in the study. Ultrasonic emulsification-solvent evaporation method is applied to combine the sustained-release microspheres material with temozolomide to form a composite sustained-release microsphere (TMZ-PLGA-W). The ratio of lactic acid (LA) and glycolic acid (GA) was adjusted so as to test the morphological characteristics of TMZ-PLGA-W at different ratios. The amount of drug released and the encapsulation rate of the material at different time periods were calculated. The C6 glioma system was implanted into the right caudate nucleus of Wistar rats to obtain a rat intracranial glioma model. The models were divided into 5 groups according to different sustained-release materials, and each group had 10 rats. The brain tumor at different times were compared and the survival time of rats was statistically calculated. The TMZ-PLGA-W sustained-release microsphere material with LA/GA ratio of 25%/75% was selected and placed in C6 cells culturing incubator according to different drug loadings. The cell activity according to the culture time was observed. The results showed that the TMZ-PLGA-W sustained-release microspheres prepared in the study were stable in structure, uniform in size, and free of cracks. At the same time, the sustained-release curve showed that the microsphere material conformed to the biodynamic law, which could reduce the burst effect and prolong the sustained release of the drug. The application of TMZ-PLGA-W sustained-release microspheres can effectively inhibit the increase in the area of brain tumors in rats, and at the same time improve the survival rate of rats. The increase in the drug loading of the microspheres can further inhibit the growth of glioma cells.