FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF DRUG DELIVERY SYSTEMS BASED TELMISARTAN ENCAPSULATED IN SILK FIBROIN NANOSPHERE’S

Objective: The aim of the present work was to formulate silk fibroin (SF) nanospheres (NS’s) for drug delivery application. The current study was designed to advance the water solubility and bio-availability of telmisartan by nanoprecipitation method. Methods: SF NS’s loaded with TS were prepared by nanoprecipitation method. The drug was dissolved in aqueous solution of SF by using acetone as a non-solvent. The prepared NS’s were then characterized by FTIR, X-ray diffraction and zeta potential, and were evaluated for its, surface morphology, %drug content, encapsulation efficiency and in vitro drug release. Results: The evaluation results of SF NS’s loaded of TS showed 74.22±0.17 % entrapment efficiency, 35.21±0.02 % of drug loading, and-4.9 mV to-13.6 mV of zeta potential due to the proper bounding of TS with the β-sheets of SF, the particle size reported was within the size range of 160-186 nm having smooth surface and were spherical in shape. The SFNS’s pattern switched from random coil to β-sheet formation on treating with acetone. FTIR and DSC studies marked no such inter-molecular interactions between SF and drug molecules. The % cumulative in vitro drug release from SF NS’s exhibited quick burst release. The in vitro cumulative drug release of SF NS’s of TS it was found that about 74% of the drug was released within 8 h and about 96% of drug released at 24 hr. The rate of drug release increased with the increase in SF ratio. Conclusion: It is believed that these SF NS’s will find potential applications in drug delivery release as drug carriers, especially poor water-soluble drugs. All these results proposed that SF NS’s are eventuality handy in various drug delivery systems

FORMULATION AND EVALUATION OF DEXTROMETHORPHAN HYDROBROMIDE CONTROLLED RELEASE HOLLOW MICROSPHERES USING NATURAL POLYMER

The objective of this study was to formulate and evaluate gastric floating dosage forms of hollow microspheres for controlled delivery of dextromethorphan hydrobromide (DBM). Hollow microspheres were prepared by emulsion polymerization method using natural polymer gelatin as release retardant and coating agent. Hollow microspheres were characterized by FT-IR, DSC, SEM, and micromeritic properties. FT-IR and DSC studies showed no chemical interaction between the drug and polymers. Hollow microspheres were evaluated for percentage yield, encapsulation efficiency and in vitro release studies. The obtained angle of repose, % Carr’s index, Hausner ratio, and tapped density values were within the limits indicating good flow properties. The surface morphology revealed that microspheres were spherical with minute pores and invert dents on the surface. Among all the formulations, F-3 of hollow microspheres showed highest drug release of 79.69±0.12% at the end of 12h which was considered as the best formulation. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer-Peppas, First-order, and Zero order to evaluate the release kinetics and mechanism of the drug release. The release kinetics indicated that drug release followed non-fickian diffusion mechanism. Results of the stability studies showed that there were no significant changes in the drug content and physical appearance.

FORMULATION AND EVALUATION OF PROBIOTIC AND PREBIOTIC LOADED PELLETS BY EXTRUSION AND SPHERONIZATION FOR IMPROVED STORAGE VIABILITY

Objective: The present study aims to prepare stains-loaded enteric-coated pellets by extrusion and spheronization technique for acidic environment protection and improve the viability of the strains during storage. Methods: Lactobacillus casei and Lactobacillus plantarum strains are proven to have various therapeutic and prophylactic uses in human beings, but low stability during storage and transit to site of action has limited their action. Pellets were prepared by incorporating probiotic strains D1-D9 (L. casei) and E1-E9 (L. plantarum) by further enteric-coating the pellets, which were evaluated for particle size, loss on drying, friability, micromeritic properties, viability, disintegration, survivability in acidic and bile juices, and stability studies for 90 d respectively. Results: The method employed for preparing the pellets showed good % yields with a particle rage of 1400-850 µm. LoD values were in the range of 3.07±0.30% to 2.13±0.11%; all the prepared pellets showed good flow properties and friability in an acceptable range. SEM images revealed that enteric-coated pellets had smooth and uniformly surfaces. The viability results ranged from 8.78±0.31 to 8.53±0.15 log CFU/g and 8.47±0.15 to 8.85±0.22 log CFU/g for both L. casei and L. plantarum enteric coated pellets, respectively. The Disintegration time for the pellets was<15 min in all the formulations. The enteric-coated probiotic pellets provided adequate protection against the acidic environment. Studies of survivability in simulated gastrointestinal conditions demonstrated that formulations D7 and E7 showed higher viability among the formulations at the end of 3 h. The stability studies showed that the formulations with a higher concentration of Inulin and pectin combination proved better viability of L. casei and L. plantarum strains in the formulation during 90 d of stability study. Conclusion: This study suggested that using extrusion and spheronization techniques can be employed to prepare pellets with prebiotics (Inulin and Pectin) which can be utilized to formulate probiotic dosage forms with improved viability in physiological conditions and real-time storage condition

A REVIEW ON THE SOLID ORAL DOSAGE FORM FOR PEDIATRICS, REGULATORY ASPECTS, CHALLENGES INVOLVED DURING THE FORMULATION, AND TOXICITY OF THE EXCIPIENTS USED IN PEDIATRIC FORMULATION

Designing an appropriate dosage form in medical treatment for the pediatric population is very challenging. The major challenges faced during designing the oral solid dosage form for pediatrics are also the prerequisites for the development of the dosage form, and they are, administering the drug according to the body weight and taste masking which is followed by other factors like the safety of excipients, size of dosage form and so on. Oral solid dosage forms like mini-tablets, soluble films, and orally disintegrating tablets are a few promising dosage forms for use in the pediatric population. The obstacles such as physiological differences between the various age groups, excipient safety, technology requirements, low profitability, clinical trial limitations, and regulatory ambiguity all have an impact on pediatric dosage form development. Recent advancement in the development of pediatrics formulations has been made due to new regulations, more financial opportunities, and novel collaborative research programs. A shift of pattern towards solid oral dosage form and an emphasis on innovative preparations, such as dispersible, flexible, as well as multi-particulate oral solid dose forms, are some of the advancements. Such advancements have allowed for more flexibility of dose, easy administration, and improved medication formulation acceptance in pediatrics. In consideration of dosage forms for pediatrics, issues such as pediatric suitability, excipient selection, prospects for modified drug release formulations or fixed-dose combinations, palatability, and acceptability, as well as challenges were reviewed in the current manuscript

Enhanced Cytotoxic Activity of Docetaxel-Loaded Silk Fibroin Nanoparticles against Breast Cancer Cells

Despite decades of research, breast cancer therapy remains a great challenge. Docetaxel is an antimicrotubule agent that is effectively used for the treatment of breast cancer. However, its clinical use is significantly hampered by its low water solubility and systemic toxicity. The current study was designed to prepare docetaxel (DXL)-loaded silk-fibroin-based nanoparticles (SF-NPs) and to screen their potential antitumor activity against breast cancer cell lines. DXL-loaded SF-NPs were prepared using a nanoprecipitation technique and were evaluated for particle size, zeta potential, entrapment efficiency, and in vitro release profile. In addition, DXL-loaded SF-NPs were screened for in vitro cytotoxicity, cellular uptake, and apoptotic potential against MCF-7 and MDA-MB-231 breast cancer cell lines. The prepared DXL-loaded SF-NPs were 178 to 198 nm in diameter with a net negative surface charge and entrapment efficiency ranging from 56% to 72%. In vitro release studies exhibited a biphasic release profile of DXL from SF-NPs with sustained drug release for 72 h. In vitro cell studies revealed that entrapment of DXL within SF-NPs significantly improved cytotoxic potential against breast cancer cell lines, compared to the free drug, and enhanced cellular uptake of DXL by breast cancer cells. Furthermore, the accumulation in the G2/M phase was significantly higher in cells treated with DXL-loaded SF-NPs than in cells treated with free DXL. Collectively, the superior antitumor activities of DXL-loaded SF-NPs against breast cancer cells, compared to free DXL, could be ascribed to improved apoptosis and cell cycle arrest. Our results highlighted the feasibility of using silk fibroin nanoparticles as a nontoxic biocompatible delivery vehicle for enhanced therapeutic outcomes in breast cancer

An Update on Emergent Nano-Therapeutic Strategies against Pediatric Brain Tumors

Pediatric brain tumors are the major cause of pediatric cancer mortality. They comprise a diverse group of tumors with different developmental origins, genetic profiles, therapeutic options, and outcomes. Despite many technological advancements, the treatment of pediatric brain cancers has remained a challenge. Treatment options for pediatric brain cancers have been ineffective due to non-specificity, inability to cross the blood–brain barrier, and causing off-target side effects. In recent years, nanotechnological advancements in the medical field have proven to be effective in curing challenging cancers like brain tumors. Moreover, nanoparticles have emerged successfully, particularly in carrying larger payloads, as well as their stability, safety, and efficacy monitoring. In the present review, we will emphasize pediatric brain cancers, barriers to treating these cancers, and novel treatment options