“… 55 As shown in Figure 2A (v), some characteristic peaks of the drug in the nanoparticles may be diminished or disappear due to encapsulation and/or weak absorption of SPL within the polymeric network. 58 Figure 2 Fourier transform infrared ( A ), Differential scanning calorimetric ( B ) thermograms, and X-ray diffraction ( C ) spectra of (i) pure SPL, (ii) PLGA, (iii) physical mixture of SPL-PLGA-PVA (PM), (iv) plain F4, and (v) medicated F4. …”
Section: Resultsmentioning
confidence: 99%
“…In the light of all FTIR, DSC, XRD data, it can be revealed that SPL-loaded PLGA nanoparticles were successfully prepared and completely dispersed/encapsulated inside the polymer matrix. 58 …”
Background
Schistosomiasis is a chronic debilitating parasitic disease accompanied with severe mortality rates. Although praziquantel (PZQ) acts as the sole drug for the management of this disease, it has many limitations that restrict the use of this treatment approach. Repurposing of spironolactone (SPL) and nanomedicine represents a promising approach to improve anti-schistosomal therapy. We have developed SPL-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) to enhance the solubility, efficacy, and drug delivery and hence decrease the frequency of administration, which is of great clinical value.
Methods
The physico-chemical assessment was performed starting with particle size analysis and confirmed using TEM, FT-IR, DSC, and XRD. The antischistosomal effect of the SPL-loaded PLGA NPs against
Schistosoma mansoni
(
S. mansoni
)-induced infection in mice was also estimated.
Results
Our results manifested that the optimized prepared NPs had particle size of 238.00 ± 7.21 nm, and the zeta potential was −19.66 ± 0.98 nm, effective encapsulation 90.43±8.81%. Other physico-chemical features emphasized that nanoparticles were completely encapsulated inside the polymer matrix. The in vitro dissolution studies revealed that SPL-loaded PLGA NPs showed sustained biphasic release pattern and followed Korsmeyer–Peppas kinetics corresponding to Fickian diffusion (
n
<0.45). The used regimen was efficient against
S. mansoni
infection and induced significant reduction in spleen, liver indices, and total worm count (
ρ
<0.05). Besides, when targeting the adult stages, it induced decline in the hepatic egg load and the small intestinal egg load by 57.75% and 54.17%, respectively, when compared to the control group. SPL-loaded PLGA NPs caused extensive damage to adult worms on tegument and suckers, leading to the death of the parasites in less time, plus marked improvement in liver pathology.
Conclusion
Collectively, these findings provided proof-of-evidence that the developed SPL-loaded PLGA NPs could be potentially used as a promising candidate for new antischistosomal drug development.
“… 55 As shown in Figure 2A (v), some characteristic peaks of the drug in the nanoparticles may be diminished or disappear due to encapsulation and/or weak absorption of SPL within the polymeric network. 58 Figure 2 Fourier transform infrared ( A ), Differential scanning calorimetric ( B ) thermograms, and X-ray diffraction ( C ) spectra of (i) pure SPL, (ii) PLGA, (iii) physical mixture of SPL-PLGA-PVA (PM), (iv) plain F4, and (v) medicated F4. …”
Section: Resultsmentioning
confidence: 99%
“…In the light of all FTIR, DSC, XRD data, it can be revealed that SPL-loaded PLGA nanoparticles were successfully prepared and completely dispersed/encapsulated inside the polymer matrix. 58 …”
Background
Schistosomiasis is a chronic debilitating parasitic disease accompanied with severe mortality rates. Although praziquantel (PZQ) acts as the sole drug for the management of this disease, it has many limitations that restrict the use of this treatment approach. Repurposing of spironolactone (SPL) and nanomedicine represents a promising approach to improve anti-schistosomal therapy. We have developed SPL-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) to enhance the solubility, efficacy, and drug delivery and hence decrease the frequency of administration, which is of great clinical value.
Methods
The physico-chemical assessment was performed starting with particle size analysis and confirmed using TEM, FT-IR, DSC, and XRD. The antischistosomal effect of the SPL-loaded PLGA NPs against
Schistosoma mansoni
(
S. mansoni
)-induced infection in mice was also estimated.
Results
Our results manifested that the optimized prepared NPs had particle size of 238.00 ± 7.21 nm, and the zeta potential was −19.66 ± 0.98 nm, effective encapsulation 90.43±8.81%. Other physico-chemical features emphasized that nanoparticles were completely encapsulated inside the polymer matrix. The in vitro dissolution studies revealed that SPL-loaded PLGA NPs showed sustained biphasic release pattern and followed Korsmeyer–Peppas kinetics corresponding to Fickian diffusion (
n
<0.45). The used regimen was efficient against
S. mansoni
infection and induced significant reduction in spleen, liver indices, and total worm count (
ρ
<0.05). Besides, when targeting the adult stages, it induced decline in the hepatic egg load and the small intestinal egg load by 57.75% and 54.17%, respectively, when compared to the control group. SPL-loaded PLGA NPs caused extensive damage to adult worms on tegument and suckers, leading to the death of the parasites in less time, plus marked improvement in liver pathology.
Conclusion
Collectively, these findings provided proof-of-evidence that the developed SPL-loaded PLGA NPs could be potentially used as a promising candidate for new antischistosomal drug development.
“…The use of hydrogel alone has been investigated by López-Cano et al, demonstrating promising results; however, its efficacy was only tested with small molecules in vitro; therefore, the stability and drug release could differ after in vivo injection, demonstrating rapid degradation or clearance as often seen for non-protected small molecules [ 84 ]. On the other hand, Suri et al studied NPs of PLGA and Chitosan to protect and deliver sirolimus to the retina for the treatment of age-related macular degeneration [ 85 ]; however, NPs alone might not ensure a prolonged release of the drug as they are often rapidly cleared from the eye, requiring multiple injections. Thus, the combination of NPs and hydrogels seems to be the most effective strategy going forward to achieve both prolonged release and protection of the drug.…”
A drawback in the development of treatments that can reach the retina is the presence of barriers in the eye that restrain compounds from reaching the target. Intravitreal injections hold promise for retinal delivery, but the natural defenses in the vitreous can rapidly degrade or eliminate therapeutic molecules. Injectable hydrogel implants, which act as a reservoir, can allow for long-term drug delivery with a single injection into the eye, but still suffer due to the fast clearance of the released drugs when traversing the vitreous and random diffusion that leads to lower pharmaceutic efficacy. A combination with HA-covered nanoparticles, which can be released from the gel and more readily pass through the vitreous to increase the delivery of therapeutic agents to the retina, represents an advanced and elegant way to overcome some of the limitations in eye drug delivery. In this article, we developed hybrid PLGA-Dotap NPs that, due to their hyaluronic acid coating, can improve in vivo distribution throughout the vitreous and delivery to retinal cells. Moreover, a hydrogel implant was developed to act as a depot for the hybrid NPs to better control and slow their release. These results are a first step to improve the treatment of retinal diseases by protecting and transporting the therapeutic treatment across the vitreous and to improve treatment options by creating a depot system for long-term treatments.
“…For decades, a large number of studies have focused on evaluating the potential of biomaterials for various applications including regenerative medicine and anti-aging. For example, in age-related macular degeneration (AMD), Suri et al for the first time delivered chitosan modified poly (lactic-co-glycolic acid) (PLGA) nanoparticles containing sirolimus to the posterior segment of the eye via the subconjunctival route for the treatment of AMD in rat models, achieving slow degradation and the necessary long-term sustained drug release while minimizing systemic exposure [ 21 ]. In addition, in age-related brain diseases, Chang et al constructed electrically magnetized gold nanoparticles (AuNPs) to improve cognitive function and memory consolidation by promoting adult hippocampal neurogenesis [ 22 ].…”
Ovarian aging is characterized by a progressive decline in ovarian function. With the increase in life expectancy worldwide, ovarian aging has gradually become a key health problem among women. Over the years, various strategies have been developed to preserve fertility in women, while there are currently no clinical treatments to delay ovarian aging. Recently, advances in biomaterials and technologies, such as three-dimensional (3D) printing and microfluidics for the encapsulation of follicles and nanoparticles as delivery systems for drugs, have shown potential to be translational strategies for ovarian aging. This review introduces the research progress on the mechanisms underlying ovarian aging, and summarizes the current state of biomaterials in the evaluation and treatment of ovarian aging, including safety, potential applications, future directions and difficulties in translation.
Graphical Abstract
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