Curcumin enriched nanoformulation: Characterization, solubility, stability and associated antioxidant, anti-inflammatory and anti-tyrosinase properties

curcumin (CUR), a natural bioactive, chiefly present in Curcuma longa L. rhizomes, exerts therapeutic potential for numerous chronic disorders by virtue of its profound anti-oxidant, anti-inflammatory and anti-tyrosinase action. Nonetheless, its therapeutic utility is hinders owing to its poor solubility, stability issues, fast metabolism, poor absorption and bioavailability issues. Polymer based nano systems have fascinated scientific community over the past few decades. As a potential polymer system, β-cyclodextrin nanosponges demonstrated the potential to entrap bioactives and aid in their solubility, stability and bioavailability. Hence, the current research work is aimed to formulate, characterize curcumin enriched nanosponges (CUR-NSs) and evaluate the anti-oxidant, anti-tyrosinase and anti-inflammatory activities. Initially, curcumin enriched nanosponges were fabricated by varying polymer: cross-linker ratios resulting in expectable entrapment, size and release profile. Besides successful characterization, solubility and photostability of CURNS4 were found enhanced in comparison to pure bioactive. Further, findings of anti-oxidant, anti-tyrosinase and anti-inflammatory activities were found promising for CUR nanosponges. In vitro release of CUR was found enhanced in CURNS4 compared to pure bioactive. Hence, findings of this research work highlight the significance of CUR enriched nanosponges to appraise its effectivenes

Cyclodextrin Nanosponges: A Promising Approach for Modulating Drug Delivery

Nanotechnology showed great promise and impact on administration of therapeutic agents owing to its advantages over contemporary delivery systems. Nanoscale carriers like nanosponges represent a novel category of hyper cross-linked polymer structures with nanosized cavities which can be filled with variety of active moieties (hydrophilic as well as hydrophobic). These nanocarriers can circulate around the body until they found the specific target site and adhere on the surface and release the active moiety in a predictable and controlled manner, resulting in more effective delivery of a given dosage. Nanosponge technology helps to reduce drug associated side effects, improve stability, increase elegance and improve the flexibility of formulations, administered orally, parenterally and topically. Among nanosponges, cyclodextrin-based nanosponges (CDNS) are smart versatile carriers studied widely for drug delivery applications. Statistically, it have presented that approximately 40% of active moieties marketed currently and about 90% of active moieties in their preliminary phase confront problems regarding to solubility. In the past decade, the number of studies describing CDNS has dramatically increased. In the present chapter, scientists working in arena of nanotechnology can get an idea of fabrication, characterization and therapeutic utilities of nanosponges

β-Cyclodextrin nanosponges for enhanced anti-melanoma potential of silymarin with functions of anti-oxidant, anti-inflammatory and anti-tyrosinase

Overproduction of inflammatory and oxidative species has been identified as key contributors for skin cancer progression. Silymarin (SLY), a natural flavonoid has demonstrated potential anti-inflammatory, anti-oxidant, anti-tyrosinase and anti-cancer activities. Nonetheless, its inherent physicochemical properties such as low solubility, low bioavailability and instability restrict its utility. Hence, current research was planned to address these challenges via encasing silymarin in nanosponges (NS) and exploring for application against skin cancer. Aiming this, silymarin was encased into NS batches prepared by melt technique and pre-eminent batch was selected on the basis of solubility, encapsulation and release. The selected batch (SLY-NS6) was suitably characterized and assessed for in-vitro DPPH scavenging, anti-inflammatory and anti-tyrosinase activities. Cell viability and apoptosis potential against B16F10 cells were performed. Further, evaluation of photostabiility was also conducted. Particle size and zeta potential of SLY-NS6 was found as 334.73 ± 79.63 nm and −29 ± 3.87 mV, respectively. The solubility and encapsulation efficiency of SLY-NS6 was 208.60 ± 13.63 µg/ml and 70.37 ± 1.04, respectively. All batches of SLY-NS has demonstrated delayed release pattern and found to follow Korsmeyer-Peppas model and Fickian diffusion mechanism. The anti-inflammatory activity of SLY and SLY-NS6 were noted 97.02% and 95.19%, respectively, at maximum concentration. The DPPH scavengingand anti-tyrosinase potential of bioactive was also found preserved after its encasement into NS. In-vitro cell viability assay of both SLY and SLY-NS6 showed concentration dependent cytotoxicity with IC50 values 118.75 µg/ml and 87.73 µg/ml, respectively. Further, it was observed that apoptosis effect of SLY-NS6 was remarkably enhanced in comparison to SLY. Photostability study revealed better protection of bioactive after its encasement. In conclusion, SLY-NS is able to address the inherent solubility and stability issues, thereby, enhancing efficacy of bioactive. Promising findings of anti-inflammatory, anti-oxidant, anti-tyrosinase and anti-cancer activities of SLY-NS advocated its potential for management skin cancer

Type 0 Spinal Muscular Atrophy in rare association with congenital contracture and generalized osteopenia: A Case Report

AbstractSpinal muscular atrophy (SMAs) is a group of rare autosomal recessive diseases in which there is degeneration of alpha motor neurons in the spinal cord leading to progressive distal motor weakness. Here we report a case of type 0 SMA in newborn with generalized osteopenia and bony deformity in form of unilateral club foot. It may be emphasized that  diagnosis of SMA should be kept in mind as a differential in cases of unexplained severe generalized hypotonia and severe respiratory compromise immediately after birth

A rare case of hyperhomocysteinemia-associated thrombotic stroke in the pediatric age group

Association between hyperhomocysteinemia and stroke has been well documented in the literature. However, there are limited reports revealing stroke events in the pediatric population affected by hyperhomocysteinemia. Herein, we present a case which shows genetically inherited hyperhomocysteinemia leading to a stroke event in a 14-year-old child. The patient presented to the outpatient clinic with dizziness and nonprojectile vomiting since the previous day without any history of weakness in the extremities or unconsciousness. The preliminary neurologic examination showed positive right-sided cerebellar signs like ataxia on physical examination and the final diagnostic workup confirmed acute non-hemorrhagic bilateral cerebellar and medullary infarction with hyperhomocysteinemia. We discuss the case presentation, diagnostic workup, and management strategies

Polycomb Repressive Complex(es) and Their Role in Adult Stem Cells

Populations of resident stem cells (SCs) are responsible for maintaining, repairing, and regenerating adult tissues. In addition to having the capacity to generate all the differentiated cell types of the tissue, adult SCs undergo long periods of quiescence within the niche to maintain themselves. The process of SC renewal and differentiation is tightly regulated for proper tissue regeneration throughout an organisms’ lifetime. Epigenetic regulators, such as the polycomb group (PcG) of proteins have been implicated in modulating gene expression in adult SCs to maintain homeostatic and regenerative balances in adult tissues. In this review, we summarize the recent findings that elucidate the composition and function of the polycomb repressive complex machinery and highlight their role in diverse adult stem cell compartments

A Fresh Look on Bergenin: Vision of Its Novel Drug Delivery Systems and Pharmacological Activities

Bergenin (BER), a key constituent of Bergenia crassifolia (Saxifragaceae), has gained extensive attention, owing to its array of pharmacological actions, including anti-infective, anti-cancer, anti-diabetic, neuroprotective, hepatoprotective, anti-urolithiatic, anti-hyperuricemic, and anti-bradykinin properties. Despite ever-intensifying support for its therapeutic features, the poor solubility, lower oral bioavailability, shorter half-life, and more intestinal pH degradation (pH 6.8 or above) of BER have puzzled researchers. To circumvent these pharmaceutical challenges, and to improve its therapeutic efficacy, newer approaches have been adopted by research scientists. Thus, a discussion of the existing literature may provide complete information about the advances in delivery strategies for enhancing its utility. This paper summarizes up-to-date works on the design and development of novel delivery carriers of this bioactive compound, such as phospholipid complexes, extended-release core tablets, prodrugs, herbal gels, polyherbal ointments, nanoparticles, and poly (lactic acid) polymers, with the objective of harnessing its full potential. This review also provides a deep insight into its bioactivities, along with mechanisms. Additionally, the physicochemical attributes, chemistry, and pharmacokinetics of BER are discussed herein. Hence, the comprehensive information documented in this review may introduce new avenues for research advancements of BER

Antibacterial, Antioxidant, Collagenase inhibition, Urease inhibition activities and Chemical composition of the Essential oil and extracts of Cinnamomum zeylanicum bark.

Significant biological activities of bacterial infection like antibacterial, antioxidant, urease and collagenase inhibitory activities of the essential oil and various extracts of Cinnamomum zeylanicum were determined. The in vitro antibacterial activity against nine epidermal bacteria and 11 MRSA isolates was conducted. The essential oil of C. zeylanicum exhibited the activity against all bacteria with the Minimum Inhibitory Concentration values (MIC) ranging from 0.15 to 2.5 µl. The extracts showed declined antibacterial activity. The scanning electron microscopic (SEM) studies demonstrated potential detrimental effect of the essential oil on the morphology of tested bacteria. Antioxidant activity of all the samples was also determined and 20% activity was observed in essential oil. Collagenase inhibitory potential  was upto 25% and 30% in aqueous and methanol extracts respectively while upto 35% in essential oil. None of the samples showed urease inhibitory activity. The chemical composition of hydrodistilled essential oil of C. zeylanicum was also analysed by GC-MS. A total of 13 compounds representing 100% of the oil were identified. Therefore, due to different chemical components present in the cinnamon essential oil, further investigation concerned with studied activities of this essential oil to replace the medicines or as supplement in diseases, is recommended

Antibacterial, Antioxidant, Collagenase inhibition, Urease inhibition activities and Chemical composition of the Essential oil and extracts of Cinnamomum zeylanicum bark.

Significant biological activities of bacterial infection like antibacterial, antioxidant, urease and collagenase inhibitory activities of the essential oil and various extracts of Cinnamomum zeylanicum were determined. The in vitro antibacterial activity against nine epidermal bacteria and 11 MRSA isolates was conducted. The essential oil of C. zeylanicum exhibited the activity against all bacteria with the Minimum Inhibitory Concentration values (MIC) ranging from 0.15 to 2.5 µl. The extracts showed declined antibacterial activity. The scanning electron microscopic (SEM) studies demonstrated potential detrimental effect of the essential oil on the morphology of tested bacteria. Antioxidant activity of all the samples was also determined and 20% activity was observed in essential oil. Collagenase inhibitory potential  was upto 25% and 30% in aqueous and methanol extracts respectively while upto 35% in essential oil. None of the samples showed urease inhibitory activity. The chemical composition of hydrodistilled essential oil of C. zeylanicum was also analysed by GC-MS. A total of 13 compounds representing 100% of the oil were identified. Therefore, due to different chemical components present in the cinnamon essential oil, further investigation concerned with studied activities of this essential oil to replace the medicines or as supplement in diseases, is recommended