PROCESS FOR PREPARING PHASE-INVERSION BASED POLYMERIC SOLUTION BY HOT-MELT EXTRUSION TECHNOLOGY
Srushti Tambe*, Purnima Amin
Institute of Chemical Technology, Department of Pharmaceutical Science and Technology, Nathalal Parekh Marg, Matunga, Mumbai, Maharashtra 400019
Poloxamers, carbomers, gellan gum, and other polymers with sol-gel phase inversion properties require overnight hydration of the polymer(s) and prolonged stirring, which results in longer processing time and several other drawbacks. The present study introduces for the first time, a novel process for preparing a phase-inversion based polymeric solution by Hot-melt extrusion technology. The proposed process is superior owing to its relatively short production time, one-step processing, continuous manufacturing, automation, real-time monitoring, and cost-effectiveness. The process presented herein makes scale-up easier as it only requires running continuous manufacturing longer and can speed up the supply chain significantly. It also overcomes the drawbacks of batch-to-batch variation and allows incorporation of QbD concepts and appropriate design of experiment methodologies to achieve consistent quality products during the large-scale production of phase-inversion based polymeric solution. The final product is of improved quality, devoid of air bubbles, better homogeneity, content uniformity, and consistency.
NOVEL DOCETAXEL LOADED VITAMIN-E-BASED MICELLES: TO ENHANCE ANTICANCER EFFICACY OF DOCETAXEL ON MDA-MB 231 CELL LINE
Harshali Dhaygude. *, Dr. Naveen Chella.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER-Hyderabad), Balanagar, Hyderabad, India – 400037
The aim of the present study was to develop Docetaxel-loaded vitamin E-based micelles (DTX– TOS–TPGS), by taking advantage of vitamin E derivatives (Tocopherol succinate (TOS) and D-a-tocopherol polyethylene glycol 1000 succinate (TPGS1000) anti-cancer property. We formulated micelles containing a mixture of TPGS (as a stabilizer) & TOS (as a solubilizer) in a 1:1 ratio. DTX–TOS–TPGS micelles a size was found to be 96.8 ± 3.79 nm, polydispersity index (PDI) of 0.217 ± 0.051, and z potential of -14.9 ± 4.25 mV. The CMC value of TOS-TPGS1000 micelles was found to be 40 µg/ mL. The Entrapment Efficiency (% EE) was found to be 70.63±3.8371%. The in-vitro drug release study has shown about 88.99 ± 2.217 % release in 6 h, 81.38 ± 2.612 % in 12 h, and 63.10 ± 2.633% in 72 h from drug dispersion, marketed Taxotere and DTX- loaded micelles respectively under similar conditions. When compared to Taxotere® and free Docetaxel, DTX-TOS-TPGS micelles achieved lower values after incubating the breast cancer cell i.e. MDA-MB 231 lines for 24-h.( on MDA-MD-231 cell line, at 24 h, was found to be 1.32 µg/mL, 8.4 µg/mL,12 µg/mL for DTX loaded micelles, marketed Taxotere® & free drug respectively). The percent hemolysis for DTX-loaded micelles and marketed Taxotere® was found to be 39.11 ± 1.336%, 64.10 ± 1.088% respectively. Micelles were found to be physically stable over one month period with a very slight increase in particle size was observed. Chemical stability showed that 87% of the drug was retained after one month period. Based on the observed results, we can conclude that the developed formulations in the present research can be taken into account as a competent drug delivery system for Docetaxel (DTX) in cancer treatment.
SYNBIOTIC PREPARATION LOADED CAPSULE FOR GUT MICROBIOTA TO TREAT ULCERATIVE COLITIS
Aishwarya Potdar *, Ashlesha Pandit
Department of Pharmaceutics, JSPM’s Rajarshi Shahu College of Pharmacy and Research, Tathawade, Pune, Maharashtra 411 033, India
Probiotics are considered to treat ulcerative colitis, wherein, addition of prebiotics provide source of food for probiotics to proliferate and increase in numbers on the bowel microflora. Current study deals with addition of both, probiotics Lactobacillus acidophilus and prebiotics inulin into sodium alginate film. Film showed good flexibility and tensile strength, which was further rolled into HPMC capsule. Next, capsule was enteric coated by dip coating technique, which prevented the rupture into stomach acidic medium and was dissolved at intestinal region, at the site of ulcerative colitis, thus, balancing the imbalanced natural microflora rather than treating with synthetic drugs.
VESICULAR NANOCARRIERS FOR DERMAL DELIVERY OF ACITRETIN – PROOF OF CONCEPT AND IN VITRO EVALUATION
Saurabh Katawale*, Preethi Naik, Mangal Nagarsenker.
Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai, Maharashtra, India- 400098
Nanoparticulate carriers like liposomes and other vesicular systems have been demonstrated to improve penetration of hydrophilic as well as lipophilic molecules across the stratum corneum. Present work provides proof of concept of a long-acting system for effective delivery of acitretin to the deeper layers of epidermis and avoiding systemic exposure. Acitretin was loaded into liposomes and studied for in vitro release using artificial membrane and in vitro permeation using rat abdominal skin. Transmission electron microscopy and differential scanning calorimetry confirmed the successful fabrication of acitretin in the two lipid vesicular nanocarriers. LeciPlex® system showed high in vitro permeation through stratum corneum and deposition into the deeper layers of skin.
DEVELOPMENT AND CHARACTERIZATION OF NANOEMULSION OF CASPOFUNGIN FOR OPHTHALMIC DRUG DELIVERY
Mercy Macwan*a, Bhupendra Prajapati b
Institute: Shree S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Mehsana-Gozaria Highway, Kherva, Ganpat Vidyanagar, Mehsana, Gujarat 384012, India.
*a Research Scholar, Shree S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Kherva.
b Professor, Shree S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Kherva.
Caspofungin is first representative of a new antifungal class belongs to the echinocandin family, that act on the fungal cell wall by inhibition of synthesis of β (1, 3)-d-glucan. Currently it is available in eye drops in market which have the limitations due to high lacrimal drainage and low corneal permeability. The aim of the present work is to optimize and characterize nano emulsion of a highly soluble drug, Caspofungin. Nanoemulsion was prepared using high shear homogenization followed by high pressure homogenizer. Solubility studies were carried out to identify suitable oil and surfactant. A three level three factor Box-Behnken design was used to optimize nano emulsion. Prepared formulation was characterized for globule size, zeta potential, polydispersity index and in vitro drug release study by dialysis method using bottle apparatus. Eye irritation study was carried out by Hen’s egg chorioallantoic Membrane test. Stability study of the prepared formulation was performed as per ICH guidelines. Prepared nanoemulsion is transparent with a blue tinge. Optimized batch of nanoemulsion showed average globule size of 111.5 nm with a poly dispersity index of 0.109. The results of in vitro drug release study suggest more than 90% drug release over a period of 24 h. Developed formulation was found to be non irritant and stable when stored at 40°C and can be used for ophthalmic delivery.