Formulation and Evaluation of Liposomal Drug Delivery System for Sulfasalazine

Aim: Aim of the current study is to prepare and characterize sulfasalazine-loaded liposomes to improve the bioavailability of the drug and to lessen the adverse effects of the drug. Background: Diseases like inflammatory bowel disease can be treated by anti-inflammatory agents like “Sulfasalazine,” It can also be used to treat ulcerative colitis and Crohn’s disease. The biological half-life of sulfasalazine is 5-10hr; as in the case of conventional therapy, there is a chance of missing the dose. Therefore, frequent administration of drugs is essential to maintain the desired steady-state level. The side effects are thrombocytopenia, megaloblastic anemia, bone marrow depression, folic acid deficiency, impairment of male fertility (Oligospermia), intestinal nephritis due to 5-ASA, diarrhoea, headache, and skin rashes. The bioavailability of sulfasalazine is 15%. This work was undertaken to enhance bioavailability and decrease the side effects. Objective: The main objective of the study is to improve the solubility of sulfasalazine by formulating a liposomal drug delivery system. The major objective is to develop a liposomal formulation with good stability and the highest entrapment efficiency. Methods: Liposomes were produced by the thin-film hydration method. Nine formulations of liposomes were prepared by varying the concentrations of soya lecithin and cholesterol and changing the drug ratio. The obtained liposomes were characterized for surface morphology, FTIR, particle size, zeta potential, drug content, entrapment efficiency, and in-vitro diffusion studies. Results: Among the nine formulations of liposomes, F3 was found to be the best formulation with an entrapment efficiency of 97.8% and a zeta potential value of -37.2mV. Liposomes followed first-order kinetics with a non-fickian diffusion pathway. Conclusions: Sulfasalazine loaded liposomes were prepared with good stability and the highest entrapment efficiency.

Application of Box–Behnken Design and Desirability Function in the Development and Optimization of Stealth Liposomes of Microtubule Inhibitor

Aims: The aim of the present study was to develop and optimize a Stealth Liposomal Drug Delivery System of microtubule inhibitor using Box–Behnken Design and Desirability function. Study Design: Development and Optimization of Stealth Liposomes. Place and Duration of Study: The study was carried out in the Department of Pharmacy, Annamalai University, between September 2020 and May 2021. Methodology: Stealth Liposomes were prepared by the thin-film hydration method (TFH). The formulation was optimized using Box – Behnken design to study the effect of independent variables, Amount of Egg Phosphatidylcholine (X1), Amount of Cholesterol (X2), and Amount of DSPE-PEG 2000(X3) on dependent variables Entrapment Efficiency (Y1) and In-vitro drug release (Y2). Results: Entrapment efficiency of the Stealth Liposomes ranges from 56.35 to 84.25%and in-vitro release ranges from 62.38 to 94.26%. The optimized formulation was found using the desirability function to get maximum entrapment with maximum drug release. The optimized formulation showed entrapment efficiency of 80.46% and in-vitro release of 90.11%. Conclusion: Stealth Liposomal Drug Delivery System for microtubule inhibitor was successfully developed and optimized using desirability function in Design Expert software by a three-factor, three level Box – Behnken design.

Challenges of Current Anticancer Treatment Approaches with Focus on Liposomal Drug Delivery Systems

According to a 2020 World Health Organization report (Globocan 2020), cancer was a leading cause of death worldwide, accounting for nearly 10 million deaths in 2020. The aim of anticancer therapy is to specifically inhibit the growth of cancer cells while sparing normal dividing cells. Conventional chemotherapy, radiotherapy and surgical treatments have often been plagued by the frequency and severity of side effects as well as severe patient discomfort. Cancer targeting by drug delivery systems, owing to their selective targeting, efficacy, biocompatibility and high drug payload, provides an attractive alternative treatment; however, there are technical, therapeutic, manufacturing and clinical barriers that limit their use. This article provides a brief review of the challenges of conventional anticancer therapies and anticancer drug targeting with a special focus on liposomal drug delivery systems.

Effect of a Low-Level Laser on Liposomal Doxorubicin Efficacy in a Melanoma Cell Line

Introduction: The cytotoxicity of chemotherapy drugs is a significant challenge in the way of surmounting cancer. Liposomal drug delivery has proven to be efficacious in increasing the function of the drugs. Its potential to accumulate drugs in the target site and enhance the efficiency of anti-cancer agents with lower doses hinders their cytotoxicity on normal healthy cells. Since the release of drugs from liposomes is not generally on a controlled basis, several studies have suggested that external stimuli including lasers could be used to induce controlled release and boost the efficiency of liposomal drug delivery systems (LDDSs). Methods: The A375 cancer cell line was used and exposed to the liposomes containing doxorubicin in the presence of a low-level laser beam to investigate its effect on the liposomal stimuli-responsiveness release and its toxicity on cancer cells. So as to achieve that goal, Annexin V/PI was employed to analyze the number of cells that underwent apoptosis and necrosis. Results: Here, we report the effect of laser irradiation on LDDSs. According to the results obtained from the annexin V/PI assay, the pattern of viability status has shifted, so that the number of pre-apoptotic cells treated with liposomal doxorubicin and a laser beam was more than that of cells treated with only liposomal doxorubicin. Conclusion: The use of stimuli-responsive LDDSs, in this case, laser-responsive, has led to favorable circumstances in the treatment of cancer, offering enhanced cancer cell cytotoxicity.

Method Development and Characterization of Liposomal Formulation of Isotretinoin

This study aims to develop a liposomal drug delivery system of isotretinoin, an acne drug-using spray drying, as a cost-effective and time-effective technique. The liposomal formulation was prepared by using spray drying; three different strategies were adopted: suspension spray drying (SSD), thin-film hydration and spray drying (TFHSD), and emulsion spray drying (ESD). Isotretinoin was 99% bound with lipid, so lipids hydrogenated soy phosphatidylcholine (HSPC), distearoyl phosphatidylglycerol (DSPG), and cholesterol were selected for the formulation development. The HSPC, DSPG, cholesterol, and isotretinoin were taken in the ratio 4 : 1 : 0.16 : 3.1 mmol. In vitro drug release studies, microscopy, drug content, and related substance characterizations were done to formulate each strategy of spray drying prepared dry liposomes of isotretinoin. Results were compared with the USP monograph of isotretinoin. It was revealed that isotretinoin's liposomal formulation using ESD was having drug release according to the USP limits. Drug content was also according to the USP requirement; no free drug crystals were found in microscopy, multivesicular vesicles were found in shape, a particle size of up 60 µ was found. The ESD technique was a successful, time-effective, and cost-effective technique for preparing a liposomal drug delivery system for isotretinoin.