This paper presents the main aspects regarding the production of biodegradable microspheres, the optimization of parameters in the drug encapsulation process, the techniques available for polymeric systems sterilization and the effects of γ-irradiation on microparticles.
The present study investigates the drug delivery potential of polymer lipid hybrid nanocomposites (Lecithmer®) composed of poly(D,L-lactide-co-glycolide (PLGA) and soya lecithin. Core-shell structure of Lecithmer was evident from cryo-TEM images. Daunorubicin (DNR) and lornoxicam (LNX)-incorporated Lecithmer nanocomposites were evaluated for anticancer and anti-inflammatory activity. DNR- and LNX-loaded Lecithmer had mean particle size of ∼335 and ∼282.7 nm, respectively. Lecithmer formulated with different cationic lipids resulted in lower particle size (∼120 nm) and positive zeta potential. Entrapment efficiency of DNR and LNX was 93.16 and 88.59 %, respectively. In vitro release of DNR from Lecithmer was slower compared to PLGA nanoparticles. DNR release from Lecithmer was significantly higher at pH 5.5 (80.96 %) as compared to pH 7.4 (55.95 %), providing advantage for selective tumor therapy. Similarly, sustained release of LNX (30 % in 10 h) was observed at pH 7.4. DNR in Lecithmer showed superior cytotoxicity on human erythroleukemic K562 cells. Pharmacokinetic study in Wistar rats with i.v. administered DNR-loaded Lecithmer showed higher volume of distribution, lower elimination rate constant, and longer half-life (81.68 L, 0.3535 h(-1), 1.96 h) as compared to DNR solution (57.46 L, 0.4237 h(-1), 1.635 h). Pharmacodynamic evaluation of orally administered LNX-loaded Lecithmer showed superior anti-inflammatory activity with maximum inhibition of 81.2 % vis-à-vis 53.57 % in case of LNX suspension. In light of these results, Lecithmer can be envisaged as a promising nanosystem for parenteral as well as oral drug delivery.
Literature data pertaining to the physicochemical, pharmaceutical, and pharmacokinetic properties of ondansetron hydrochloride dihydrate are reviewed to arrive at a decision on whether a marketing authorization of an immediate release (IR) solid oral dosage form can be approved based on a Biopharmaceutics Classification System (BCS)-based biowaiver. Ondansetron, a 5HT 3 receptor antagonist, is used at doses ranging from 4 mg to 24 mg in the management of nausea and vomiting associated with chemotherapy, radiotherapy, and postoperative treatment. It is a weak base and thus exhibits pH-dependent solubility. However, it is able to meet the criteria of "high solubility" as well as "high permeability" and can therefore be classified as a BCS class I drug. Furthermore, ondansetron hydrochloride 8 mg IR tablets (Zofran ® 8 mg) and multiples thereof (16 mg ¼ Zofran ® 8 mg  2 tablets and 24 mg ¼ Zofran ® 8 mg  3 tablets) meet the criteria of "rapidly dissolving" in dissolution testing. Ondansetron hydrochloride has a wide therapeutic window and is well-tolerated after oral administration. Based on its favorable physicochemical properties, pharmacokinetic data and the minimal risks associated with an incorrect bioequivalence decision, the BCS-based biowaiver procedure can be recommended for ondansetron hydrochloride dihydrate IR tablets.
Vibrating mesh nebulizers (VMN) demonstrate improved efficiency for delivery of inhaled aerosol solutions or suspensions as compared to compressor devices. The added advantages of compactness, portability and functioning as noise-free device makes them of incremental value in Home or Ambulatory settings while managing Severe Obstructive airway disease or delivery of maintenance medications in these cases. This further circumvents the need for multiple devices thereby further improving patient compliance and convenience while delivering acute or maintenance formulations including Glycopyrronium (GLY) and Formoterol (FRM)/Budesonide(BUD) nebulizing solution formulations. To further assess the clinical role and feasibility of FRM-BUD formulation delivery kinetics with or without GLY nebulizing solution through VMN and jet nebulizers for In- & outpatient settings, 2 comparative in-vitro lung deposition studies were carried out utilizing Anderson Cascade impactor at 30 L/min; deposited drug concentrations in different stages were suitably collected and estimated by HPLC. Post-hoc analyses with p<0.05 was considered statistically significant for intergroup differences on FRM/BUD and GLY delivered through VMN or Compressor devices. The calculated mean fine particle dose for FRM & BUD delivered by VMN or jet nebulizer showed no statistical difference. However the mean fine particle fraction for BUD delivered by VMN was significantly better compared to jet nebulizer than that for FRM. The Residual volume at 10 mins was significantly higher with jet nebulizer. The optimal APSD for GLY nebulizing solution admixture with FRM/BUD suspension delivered through VMN and Jet nebulizer offers a clinically relevant strategy for High risk COPD cases in Acute or Home settings.
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