Ameliorating the antitumor activity of lenalidomide using PLGA nanoparticles for the treatment of multiple myeloma

Abstract Lenalidomide (LND) is an anti-cancer drug and an effective derivative of thalidomide used for multiple myeloma therapy. Because of its poor solubility in water, LND is known to cause low oral bioavailability (below 33%), and as a direct consequence of this, the dosing frequency is extended thus increasing risk of toxicity. To improve its bioavailability and sustained release, the present study aims to formulate polymeric nanoparticles (NPs) for LND using [Poly (lactic-co-glycolic acid)] (PLGA) as a polymer. The polymeric NPs were evaluated for particle size, SEM, XRD, drug content, entrapment efficiency (EE), in vitro release studies and in vivo bioavailability studies in rats. The formulated NPs possessed a size of 179±0.9 nm and a zeta potential of -24.4 ± 0.2 mV. The drug loading and EE of the optimized formulation was 32 ± 0.37 % and 78 ± 0.92% respectively. After oral administration of LND PLGA-NPs, the relative bioavailability was enhanced about 3.67-fold compared to LND. This study demonstrates the novel drug delivery for LND with PLGA-NPs as effective drug delivery system for sustained delivery of LND

Ameliorating the antitumor activity of lenalidomide using PLGA nanoparticles for the treatment of multiple myeloma

Abstract Lenalidomide (LND) is an anti-cancer drug and an effective derivative of thalidomide used for multiple myeloma therapy. Because of its poor solubility in water, LND is known to cause low oral bioavailability (below 33%), and as a direct consequence of this, the dosing frequency is extended thus increasing risk of toxicity. To improve its bioavailability and sustained release, the present study aims to formulate polymeric nanoparticles (NPs) for LND using [Poly (lactic-co-glycolic acid)] (PLGA) as a polymer. The polymeric NPs were evaluated for particle size, SEM, XRD, drug content, entrapment efficiency (EE), in vitro release studies and in vivo bioavailability studies in rats. The formulated NPs possessed a size of 179±0.9 nm and a zeta potential of -24.4 ± 0.2 mV. The drug loading and EE of the optimized formulation was 32 ± 0.37 % and 78 ± 0.92% respectively. After oral administration of LND PLGA-NPs, the relative bioavailability was enhanced about 3.67-fold compared to LND. This study demonstrates the novel drug delivery for LND with PLGA-NPs as effective drug delivery system for sustained delivery of LND

Understanding the implications of pharmaceutical excipients and additives in the treatment of diabetic foot ulcers

A diabetic foot ulcer (DFU) is a consequence of Diabetes Mellitus (DM) and involves complex pathological processes. Among diabetic patients DFU is a major cause of deaths resulting from the amputation of the lower limbs. Various treatment strategies have been developed for the treatment of DFUs, but to this date unfortunately no single treatment fulfills the prerequisites necessary for treating this condition due to its complex, multifactorial pathophysiology. Additionaly, costs associated with the treatment can be prohibitively high. Excipients are pharmaceutical agents which have diverse applications in the design of different dosage forms. Therefore, an ideal dosage form, with active excipients in combination or as adjuvants, which meet these requirements could be suited for treating DFUs. This review discusses the etiopathogenesis of DFUs and also the possible of the use of excipients and additives in various pathological cases of DFUs in designing medicinal products intended for the treatment of this condition

Understanding the implications of pharmaceutical excipients and additives in the treatment of diabetic foot ulcers

A diabetic foot ulcer (DFUs) is a consequence of Diabetes Mellitus (DM) and involves complex pathological processes. It is a major cause of deaths among diabetic patients as a result of amputations. Various treatment strategies have been developed for the treatment of DFUs; unfortunately no single treatment will fulfill the prerequisites necessary for treating DFUs due to its complexed, multifactorial pathophysiology and also the overall cost of these treatments are high. Excipients are the pharmaceutical agents which have diverse applications in the design of different dosage forms. Hence, an ideal dosage form, with active excipients in combination or as adjuvants, which meets these requirements would probably best suited for treating DFUs. This review discusses the etiopathogenesis of DFUs and also the possible use of excipients and additives on various pathological cases of DFUs in designing products intended for the treatment of DFUs

5-Aminosalicylic Acid attenuates allergen-induced airway inflammation and oxidative stress in asthma

Pro-inflammatory cytokines regulate the magnitude of allergic reactions during asthma. Tumor necrosis factor – alpha (TNF-α), interleukin-6 (IL-6) and interleukin-13 (IL-13) play a crucial role in aggravating the inflammatory conditions during allergic asthma. In addition, oxidative stress contributes to the pathogenesis of asthma by altering the physiological condition resulting in the development of status asthmaticus. Anti-inflammatory corticosteroids are being widely used for treating allergic asthma. In the present study 5-aminosalicylic acid (5-ASA), a salicylic acid derivative, was evaluated, in vivo for its potential to suppress TNF-α, IL-6 and IL-13 using ovalbumin (OVA) induced allergic asthma in Balb/C mice. Oral administration of 65, 130 and 195 mg/kg 5-ASA significantly reduced the OVA induced total and differential leucocyte count, TNF-α, IL-6, IL-13, nitrite, nitrate, MDA, MPO and TPL levels in the lung lavage samples. Collectively, these findings suggest that 5-ASA is a potent immunomodulator and suppresses key Th2 cytokines production and oxidative stress in OVA-induced asthma