Formulation and optimization of sildenafil citrate-loaded PLGA large porous microparticles using spray freeze-drying technique: A factorial design and in-vivo pharmacokinetic study

Shahin, Hend I.; Vinjamuri, Bhavani Prasad; Mahmoud, Azza A.; Mansour, Suzan M.; Chougule, Mahavir B.; Chablani, Lipika

doi:10.1016/j.ijpharm.2021.120320

Cited by 22 publications

(5 citation statements)

References 51 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A major drawback of this technique is the poor encapsulation efficiency of hydrophilic components due to the partitioning of water-soluble molecules into the external aqueous phase (W2) before the formation of PLGA microspheres. As a result, several recent studies have shifted to spray drying, 23,24 spray freeze-drying, 25,26 and electrospray drying 27,28 as alternative microencapsulation techniques. The spray drying technique is a specifically designed method often used in the pharmaceutical industries to prepare drug powder with precise size and shape in bulk amounts.…”

Section: Preparation Of Plga Npsmentioning

confidence: 99%

Progress in the drug encapsulation of poly(lactic-co-glycolic acid) and folate-decorated poly(ethylene glycol)–poly(lactic-co-glycolic acid) conjugates for selective cancer treatment

et al. 2022

View full text Add to dashboard Cite

show abstract

Section: Preparation Of Plga Npsmentioning

confidence: 99%

Progress in the drug encapsulation of poly(lactic-co-glycolic acid) and folate-decorated poly(ethylene glycol)–poly(lactic-co-glycolic acid) conjugates for selective cancer treatment

et al. 2022

View full text Add to dashboard Cite

show abstract

“…Shahin et al . [ 114 ] used the same drug, material and similar technique to obtain MPs and showed that the composition of the formulation is crucial in terms of EE—the results ranged from around 3 to around 95% due to simple changes in manufacturing conditions. Furthermore, it was shown in vivo that this DDS would lead to much higher concentrations in the lungs than commercially available sildenafil for oral administration.…”

Section: Mps Based On Synthetic Polymersmentioning

confidence: 99%

Inhalable microparticles as drug delivery systems to the lungs in a dry powder formulations

Knap

Kwiecień

Reczyńska-Kolman

et al. 2022

Regenerative Biomaterials

View full text Add to dashboard Cite

Inhalation-administrated drugs remain an interesting possibility of addressing pulmonary diseases. Direct drug delivery to the lungs allows one to obtain high concentration in the site of action with limited systemic distribution, leading to a more effective therapy with reduced required doses and side effects. On the other hand, there are several difficulties in obtaining a formulation that would meet all the criteria related to physicochemical, aerodynamic, and biological properties, which is the reason why only very few of the investigated systems can reach the clinical trial phase and proceed to everyday use as a result. Therefore, we focused on powders consisting of polysaccharides, lipids, proteins, or natural and synthetic polymers in the form of microparticles that are delivered by inhalation to the lungs as drug carriers. We summarized the most common trends in research today to provide the best dry powders in the right fraction for inhalation that would be able to release the drug before being removed by natural mechanisms. This review paper addresses the most common manufacturing methods with novel modifications, pros and cons of different materials, drug loading capacities with release profiles, and biological properties such as cytocompatibility, bactericidal, or anticancer properties.

show abstract

“…The tracheal intubation technique was carried out as previously discussed. 40,41 Prior to the intubation, the rats were anesthetized intra-peritoneally using thiopental (50 mg/ kg) which was safe and enough to perform the experiment. The 1st group received pre-sterilized curcumin powder (curcumin mixed with HPβCD) as a control.…”

Section: Dose Administrationmentioning

confidence: 99%

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

Adel

ElMeligy

Abdelrahim

et al. 2021

IJN

View full text Add to dashboard Cite

Purpose The goal was to directly deliver curcumin, a natural polyphenolic anticancer and anti-inflammatory compound, to the lung tissues with minimal systemic exposure through the fabrication of proliposomes, overcoming its poor aqueous solubility and oral bioavailability. Methods Nano-spray drying was employed to prepare proliposomes using hydroxypropyl beta-cyclodextrin as a carrier. Lecithin and cholesterol were used as lipids, stearylamine and Poloxamer 188 were added as positive charge inducer and a surfactant, respectively. Different characterization parameters were evaluated like percentage yield, entrapment efficiency, drug loading, aerodynamic particle size, in vitro release besides morphological examination. Cytotoxicity studies on cell line A549 lung tumor cells as well as in vivo lung pharmacokinetic studies were also carried. Results The optimized formulations showed superior aerosolization properties coupled their enhanced ability to reach deep lung tissues with a high % of fine particle fraction. Cytotoxicity studies using MTT assay demonstrated enhanced growth inhibitory effect on lung tumor cells A549 and significant reduction of proinflammatory cytokines such as tumor necrosis factor-α, interleukin-6 and interleukin-10 compared to the pure drug. Results of lung pharmacokinetic tests confirmed the superiority of proliposomal curcumin over curcumin powder in both, the rate and extent of lung tissue absorption, as well as the mean residence time within the lung tissues. Conclusion The pulmonary delivery of curcumin-loaded proliposomes as dry powder provides a direct approach to lung tissues targeting while avoiding the limitations of the oral route and offering a non-invasive alternative to the parenteral one.

show abstract

Formulation and optimization of sildenafil citrate-loaded PLGA large porous microparticles using spray freeze-drying technique: A factorial design and in-vivo pharmacokinetic study

Cited by 22 publications

References 51 publications

Progress in the drug encapsulation of poly(lactic-co-glycolic acid) and folate-decorated poly(ethylene glycol)–poly(lactic-co-glycolic acid) conjugates for selective cancer treatment

Progress in the drug encapsulation of poly(lactic-co-glycolic acid) and folate-decorated poly(ethylene glycol)–poly(lactic-co-glycolic acid) conjugates for selective cancer treatment

Inhalable microparticles as drug delivery systems to the lungs in a dry powder formulations

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

Contact Info

Product

Resources

About