Haloperidol-loaded PLGA nanoparticles: Systematic study of particle size and drug content

Aim: EPAS (evaporative precipitation into aqueous solution) was used in the current studies to prepare azithromycin nanosuspensions and investigate the physicochemical characteristics for the nanosuspension batches with the aim of enhancing the dissolution rate of the nanopreparation to improve bioavailability. Methods: EPAS method used in this study for preparing azithromycin nanosuspension was achieved through developing an in-house instrumentation method. Particle size distribution was measured using Zetasizer Nano S without sample dilution. Dissolved azithromycin nanosuspensions were also compared with raw azithromycin powder and commercially available products. Total drug content of nanosuspension batches were measured using an Ultra-Performance Liquid Chromatography (UPLC) system with Photodiode Array (PDA) detector while residual solvent was measured using gas chromatography (GC). Results: The average particle size of azithromycin nanosuspension was 447.2 nm and total drug content was measured to be 97.81% upon recovery. Dissolution study data showed significant increase in dissolution rate for nanosuspension batch when compared to raw azithromycin and commercial version (microsuspension). The residual solvent found for azithromycin nanosuspension is 0.000098023 mg/ mL or 98.023 ppb. Conclusion: EPAS was successfully used to prepare azithromycin nanoparticles that exhibited significantly enhanced dissolution rate. Further studies are required to scale up the process and determine long term stability of the nanoparticles.

Download Full-text

Effect of Chitosan Coating on PLGA Nanoparticles for Oral Delivery of Thymoquinone: In Vitro, Ex Vivo, and Cancer Cell Line Assessments

Coatings ◽

10.3390/coatings11010006 ◽

2020 ◽

Vol 11 (1) ◽

pp. 6

Author(s):

Sultan Alshehri ◽

Syed Sarim Imam ◽

Md Rizwanullah ◽

Khalid Umar Fakhri ◽

Mohd Moshahid Alam Rizvi ◽

...

Keyword(s):

Breast Cancer ◽

Particle Size ◽

Oral Delivery ◽

Ex Vivo ◽

Cancer Cell Line ◽

Entrapment Efficiency ◽

Plga Nanoparticles ◽

Cancer Management ◽

Mcf 7

In the present study, thymoquinone (TQ)-encapsulated chitosan- (CS)-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were formulated using the emulsion evaporation method. NPs were optimized by using 33-QbD approach for improved efficacy against breast cancer. The optimized thymoquinone loaded chitosan coated Poly (d,l-lactide-co-glycolide) nanoparticles (TQ-CS-PLGA-NPs) were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA-MB-231 and MCF-7 cell lines. The surface coating of PLGA-NPs was completed by CS coating and there were no significant changes in particle size and entrapment efficiency (EE) observed. The developed TQ-CS-PLGA-NPs showed particle size, polydispersibility index (PDI), and %EE in the range between 126.03–196.71 nm, 0.118–0.205, and 62.75%–92.17%. The high and prolonged TQ release rate was achieved from TQ-PLGA-NPs and TQ-CS-PLGA-NPs. The optimized TQ-CS-PLGA-NPs showed significantly higher mucoadhesion and intestinal permeation compared to uncoated TQ-PLGA-NPs and TQ suspension. Furthermore, TQ-CS-PLGA-NPs showed statistically enhanced antioxidant potential and cytotoxicity against MDA-MB-231 and MCF-7 cells compared to uncoated TQ-PLGA-NPs and pure TQ. On the basis of the above findings, it may be stated that chitosan-coated TQ-PLGA-NPs represent a great potential for breast cancer management.

Download Full-text

Remote-Controllable Bone-Targeted Delivery of Estradiol For the Treatment of Ovariectomy-Induced Osteoporosis in Rats

10.21203/rs.3.rs-628262/v1 ◽

2021 ◽

Author(s):

Dehao Fu ◽

Yuanyuan Guo ◽

Yongwei Liu ◽

Chen Shi ◽

Tingting Wu ◽

...

Keyword(s):

Particle Size ◽

Bone Tissue ◽

Targeted Delivery ◽

Hormone Replacement ◽

Plga Nanoparticles ◽

Raw 264.7 Cells ◽

Diffusion Method ◽

Tissue Destruction ◽

Trap 5B ◽

Post Menopausal

Abstract BackgroundOsteoporosis (OP) is a systemic skeletal disease marked by bone mass reduction and bone tissue destruction. Hormone replacement therapy is an effective treatment for post-menopausal OP, but estrogen has poor tissue selectivity and severe side effects.ResultsIn this study, we constructed a poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs)-based drug delivery system to co-load 17β estradiol (E2) and iron oxide (Fe3O4) together, modified with alendronate (AL) to achieve bone targeting and realize a magnetically remote-controllable drug release. The NPs were fabricated through the emulsion solvent diffusion method. The particle size was approximately 200 nm while the encapsulation efficiency of E2 was 58.34 ± 9.21%. The NPs were found to be spherical with a homogenous distribution of particle size. The NPs showed good stability, good biocompatibility, high encapsulation ability of E2 and excellent magnetic properties. The NPs could be effectively taken up by Raw 264.7 cells and were effective in enriching drugs in bone tissue. The co-loaded NPs exposed to an external magnetic field ameliorated OVX-induced bone loss through increased BV/TV, decreased Tb.N and Tb.Sp, improved bone strength, increased PINP and OC, and downregulated CTX and TRAP-5b. The haematological index and histopathological analyses displayed the NPs had less side effects on non-skeletal tissues.ConclusionsThis study presented a remote-controlled release system based on bone-targeted multifunctional NPs and a new potential approach to bone-targeted therapy of OP.

Download Full-text

EVALUATION OF STABILITY OF ROPINIROLE HYDROCHLORIDE AND PRAMIPEXOLE DIHYDROCHLORIDE MICROSPHERES AT ACCELERATED CONDITION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i4.26184 ◽

2018 ◽

Vol 10 (4) ◽

pp. 82

Author(s):

Koyel Kar ◽

R. N. Pal ◽

Gouranga Nandi

Keyword(s):

Particle Size ◽

Drug Release ◽

Surface Morphology ◽

Shelf Life ◽

Stability Study ◽

In Vitro Drug Release ◽

Drug Content ◽

Ropinirole Hydrochloride ◽

Pramipexole Dihydrochloride

Objective: The objective of the present work was to conduct accelerated stability study as per international council for harmonisation (ICH) guidelines and to establish shelf life of controlled release dosage form of ropinirole hydrochloride and pramipexole dihydrochloride microspheres for a period of 6 mo.Methods: Most optimized batch of ropinirole hydrochloride and pramipexole dihydrochloride (F12 and M12 respectively) were selected and subjected to exhaustive stability testing by keeping the sample in stability oven for a period of 3 and 6 mo. Various parameters like surface morphology, particle size, drug content, in vitro drug release and shelf life were evaluated at 3 and 6 mo period. The surface morphology of the formulated microspheres was determined by scanning electron microscopy (SEM). The particle size of the microspheres was estimated by optical microscopy method. The drug content was assayed by the help of ultra-violet spectrophotometer (UV). The in vitro drug release was performed by using Paddle II type dissolution apparatus and the filtrate was analyzed by UV spectrophotometer. The shelf life of the optimized microspheres was calculated by using the rate constant value of the zero-order reaction.Results: A minor change was recorded in average particle size of F12 and M12 microspheres after storage for 6 mo. For F12 and M12, initially the particle size was 130.00 µm and 128.92 µm respectively and after 6 mo it was found to be 130.92 µm and 128.99 µm respectively. There was no change in surface morphology of F12 and M12 microspheres after 6 mo of storage. The shape of microspheres remained spherical and smooth after 6 mo. An insignificant difference of drug content was recorded after 6 mo compared to the freshly prepared formulation. For F12 and M12, 94.50% and 93.77% of the drug was present initially and after 6 mo 94.45% and 93.72% of the drug was recorded. In vitro drug release was recorded after 6 mo for F12 and M12. Initially, 97.99% and 97.69% of the drug was released till 14th hour respectively for F12 and M12. After 6 mo, 98.23% and 97.99% of the drug was released respectively. The percentage residual drug content revealed that the degradation of microspheres was low. Considering the initial percentage residual drug content as 100%, 99.94% of the drug was recorded for both F12 and M12. The shelf life for F12 and M12 was found to be 10 y 52 d and 10 y 70 d respectively which were determined by the zero-order kinetic equation.Conclusion: A more or less similar surface morphology, particle size, drug content and percent of drug release before and after stability study confirmed the stability of F12 and M12 microspheres after storage for 6 mo and prove the efficacy of the microspheres in the site-specific delivery of drugs in Parkinson’s disease.

Download Full-text

FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES

INDIAN DRUGS ◽

10.53879/id.55.02.10717 ◽

2018 ◽

Vol 55 (02) ◽

pp. 27-35

Author(s):

A. A Bakliwal ◽

◽

D. S. Jat ◽

S. G. Talele ◽

A. G. Jadhav

Keyword(s):

Particle Size ◽

Drug Release ◽

Release Kinetics ◽

Synthesis Method ◽

Ultra Sound ◽

Size Analysis ◽

Release Kinetic ◽

In Vitro Drug Release ◽

Drug Content

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

Download Full-text

Preparation of All-Trans-Retinoic Acid-Loaded mPEG-PLGA Nanoparticles Using Microfluidic Flow-Focusing Device for Controlled Drug Delivery

NANO ◽

10.1142/s1793292020501015 ◽

2020 ◽

Vol 15 (08) ◽

pp. 2050101

Author(s):

Mojdeh Safari ◽

Amir Amani ◽

Tajudeen Adebileje ◽

Jafar Ai ◽

Seyed Mahdi Rezayat ◽

...

Keyword(s):

Particle Size ◽

Retinoic Acid ◽

Plga Nanoparticles ◽

Process Conditions ◽

Flow Focusing ◽

Flow Rates ◽

Trans Retinoic Acid ◽

All Trans Retinoic Acid ◽

Microfluidic Flow ◽

Minimum Particle Size

In recent years, microfluidic devices present unique advantages for the development of a new generation of nanoparticle synthesis method compared to bulk methods. In this study, we report a microfluidic flow-focusing method for the production of all trans retinoic acid (ATRA)-loaded methoxy poly(ethylene glycol)-poly(lactide-coglycolide) (mPEG-PLGA) nanoparticles (NPs). Box–Behnken experimental design (BBD) was applied to optimize of formulation ingredients and process conditions with minimum particle size, maximum drug loading% (DL%) and encapsulation efficiency% (EE%). Polymer concentration, drug concentration and flow rates of solvent (S) and antisolvent (AS) were selected as independent variables. Based on optimization strategy, minimum particle size achieved shows average (SD) particle size of [Formula: see text][Formula: see text]nm with DL of [Formula: see text][Formula: see text]wt.% and EE of [Formula: see text][Formula: see text]wt.%, respectively. While maximum DL has been reported to be [Formula: see text][Formula: see text]wt.% with particle size of [Formula: see text][Formula: see text]nm and EE of [Formula: see text][Formula: see text]wt.%, respectively. Moreover, the results have shown that the AS/S ratio represents the most significant effect on particle size. Indeed, increasing the AS flow rate directly results in generating smaller particles. The AS/S ratio represents the least significant effect on DL%, such that, at fixed flow rates, higher DL was observed at high concentration of drug and lower concentration of polymer. In conclusion, optimization of the ATRA-loaded mPEG-PLGA NPs by BBD yielded in a favorable drug carrier for ATRA that could provide a new treatment modality for different malignancies.

Download Full-text

FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11s4.31721 ◽

2018 ◽

Vol 11 ◽

Author(s):

Somasundaram I

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Burst Release ◽

Drug Content ◽

Pramipexole Dihydrochloride ◽

Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

Download Full-text