The present investigation demonstrates the preparation of solid self nanoemulsfying drug delivery system (sSNEDDS) to enhance stability and bioavailability of Erlotinib (ERL) via the oral route. Capmul®MCM EP (CPM EP, oil), Cremophor® RH 40 (CMR RH 40, surfactant), and LBF CS (LBF CS, cosurfactant) were chosen as chief components for preparing Liquids SNEDDS (L-ERL-SNEDDS) based on solubility and emulsion forming ability. Pseudo ternary phase diagram and constrained mixture designs were applied to identify the self-emulsifying area and it was found that CPM EP, CMR RH 40, and LBF CS in the ratio of 59:11:30 showed optimized particle size (110.08 nm), with narrow PDI (0.114) and high ERL loading capacity (14.31 mg/g). Adsorption method was implemented for solidification of L-ERL-SNEDDS. Among various solid carriers were studied, Aerosil® 200 (A200) was finalized based on free flowing property and reconstitution ability. DSC and XRD studies revealed that crystallinity of drug was reduced in developed system. The developed formulation (named as, A200-ERL-sSNEDDS) showed increased cytotoxicity and apoptosis in PANC-1 and MIA PaCa-2 cells. Pharmacokinetic studies revealed ∼2.2 times increase in AUC0-∞values in case of A200-ERL-sSNEDDS as compared to free ERL. Thus current strategy can be extrapolated for delivering of poorly soluble drugs via oral route.
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http://dx.doi.org/10.1016/j.ijpharm.2022.121852 | DOI Listing |
J Biomater Sci Polym Ed
November 2024
Scientist- Formulation and Process Development, Strides Pharma Inc, Chestnut Ridge, NY, USA.
Erlotinib, a potent epidermal growth factor receptor (EGFR) inhibitor, faces bioavailability challenges due to poor water solubility and stability. This study aims to optimize erlotinib-loaded PLGA nanoparticles using a 3 factorial design to enhance drug delivery and therapeutic efficacy. The effects of PLGA concentration (R1) and NaTPP concentration (R2) on nanoparticle characteristics, including particle size, zeta potential, and polydispersity index (PDI), were investigated.
View Article and Find Full Text PDFInt J Pharm
December 2024
Department of Molecular Medicine, Princess Al-Jawhara Centre for Molecular Medicine, School of Medicine and Medical Sciences Arabian Gulf University, Manama 329, Bahrain. Electronic address:
Int J Pharm
October 2024
Department of Pharmaceutics, School of Pharmaceutical Sciences, Delhi Pharmaceutical Sciences and Research University (DPSRU), New Delhi 110017, India; Centre for Advanced Formulation and Technology, Delhi Pharmaceutical Sciences and Research University (DPSRU), New Delhi 110017, India. Electronic address:
This study investigates the biodistribution of a nano lipid carrier system (NLCs) containing the hydrophobic drug erlotinib (ERL-NLCs). The system was labelled with the fluorescent dye IR-780 for real-time dynamic imaging. ERL-NLCs were initially developed using the ultrasonication method with oleic acid and stearic acid.
View Article and Find Full Text PDFEur J Med Chem
October 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470, Eskişehir, Turkey. Electronic address:
In search of small molecules for targeted therapy of non-small cell lung carcinoma (NSCLC), an efficient four-step synthetic route was followed for the synthesis of new imidazothiazole-hydrazone hybrids, which were assessed for their cytotoxic effects on human lung adenocarcinoma (A549) and human lung fibroblast (CCD-19Lu) cells. Among them, compounds 4, 6, 13, 16, 17 and 21 exhibited selective cytotoxic activity against A549 cell line. In vitro mechanistic studies were performed to assess their effects on apoptosis, caspase-3, cell cycle, EGFR and Akt in A549 cells.
View Article and Find Full Text PDFEur J Pharm Biopharm
August 2024
Department of Pharmaceutical Engineering & Technology, IIT (BHU), Varanasi 221005, India. Electronic address:
The goal of the study was to fabricate folic acid functionalized docetaxel (DOC)/erlotinib (ERL)-loaded solid lipid nanoparticles (SLNs) to synergistically increase the anticancer activity against triple-negative breast cancer. DOC/ERL-SLNs were prepared by the high shear homogenization - ultrasound dispersion method (0.1 % w/v for DOC, and 0.
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