Novel Formulation Approaches used for the Management of Osteoarthritis: A Recent Review.

BACKGROUND: Osteoarthritis (OA) causes economic, social, and health difficulties in patients. Approximately 10% to 15% of all persons above the age of 60 have some degree of OA. OA is more common in women than in males. Diagnosed OA prevalence varies widely among EU member states, from 2.8% in Romania to 18.3% in Hungary. INTRODUCTION: Osteoarthritis (OA) is a slow-progressing, non-inflammatory disorder. This disorder ultimately destroys articular cartilage and other joint components. The main symptoms are stiffness, pain, loss of flexibility, swelling, and bone spurs. Many modifiable and non-modifiable risk factors have been associated with osteoarthritis (OA), including obesity and lack of exercise, genetic susceptibility, bone density, work-related damage, and trauma. METHODS: Hydrogels, micro and nano-sized particles, and novel topical gels are the most common examples. Hydrogels are cross-linked polymers with 3-D architecture that can hold water and expand like living tissue. The micro-carriers and nano-based drug delivery systems provide several advantages and may demonstrate prolonged release, controlled release, and higher joint half-life. RESULTS: OA-induced male Lewis rats were injected with celecoxib-loaded PEA microspheres to assess in vivo biocompatibility and degradation. According to the findings of this research, PEA microspheres loaded with celecoxib may be employed as safe delivery of drugs with self-regulating behavior for pain treatment related to knee osteoarthritis. CONCLUSION: The concept of novel drug delivery systems has shown tangible benefits as a new avenue for precise, safe, high-quality drug delivery for OA treatment. Currently, herbal drugs are also used in osteoarthritis treatment due to their potency and fewer side effects than synthetic drugs. The herbosynthetic approach is a new concept for the delivery of both herbal and synthetic drugs together to exploit their individual beneficial effects while reducing undesirable side effects.

A Recent Review on Bio-availability Enhancement of Poorly Water-soluble Drugs by using Bioenhancer and Nanoparticulate Drug Delivery System.

BACKGROUND: Intravenous route of drug administration has maximum bioavailability, which shows 100% of the drug reaches blood circulation, whereas the oral administration of drugs, are readily undergoing pre-systemic metabolism, which means the poor bioavailability of the drug and limited amount of drug reaches the target site. INTRODUCTION: Bioenhancers are substances having medicinal entities which enhance the bioavailability and efficacy of the active constituents of drugs. The enhanced bioavailability of drugs may lead to dose reduction, which may further reduce the cost and undesired side effects associated with the drugs. METHODS: The solid lipid nanoparticles (SLNs) loaded with ketoprofen made from carnauba wax and beeswax. It was discovered that when the drug-loaded SLNs were mixed with egg-lecithin and Tween-80, as well as when the total surfactant concentration was increased, the average particle size of the drug-loaded SLNs decreased. RESULTS: The drug-loaded nanoparticles, when given in combination with bio-enhancers such as piperine and quercetin, enhanced the drug's effectiveness. The Area Under Curve (AUC) was increased when the drug was coupled with bio-enhancers. Based on the findings, it can be concluded that piperine and quercetin when used with drug-loaded nanoparticles improve their therapeutic effectiveness. CONCLUSION: Bioenhancers are crucial to amplifying the bioavailability of many synthetic drugs. These attributes are useful to reduce the dose of drugs and increase the therapeutic efficacy of drugs with poor bioavailability.

Development and In Vivo Evaluation of Pectin Based Enteric Coated Microparticles Loaded with Mesalamine and Saccharomyces boulardii for Management of Ulcerative Colitis.

Mesalamine is the first-line choice of drug for ulcerative colitis management. However, due to the nontargeted delivery of mesalamine, it shows side effects. The possible impact of mesalamine can be improved by coated microparticles in combination with S. boulardii for targeted delivery to the colon with the prevention of unwanted side effects. In this work, pectin-based mesalamine and S. boulardii loaded microparticles were prepared by dehydration technique and coated by an oil-in-oil solvent evaporation method and characterized by Scanning electron microscopy (SEM), X-ray diffraction, and zeta analysis. 2, 4, 6-Trinitrobenzenesulfonic acid was used for the induction of colitis. The anti-inflammatory effects of coated microparticles on Caco-2 cells were assessed by the determination of interleukin (IL)-8 concentration. In addition, the impact of coated microparticles on the concentration of colonic enzymes, including myeloperoxidase (MPO), lipid peroxides, and glutathione (GSH), were also evaluated. Moreover, hematological parameters, including white blood cell (WBC), erythrocyte sedimentation rate (ESR), and C-reactive protein (CRP), were assessed. SEM data revealed that all the prepared coated microparticles had an almost spherical shape. The X-ray powder diffraction analysis of uncoated and coated microparticles showed maximum stability without any interaction. The particle size of uncoated and coated microparticles was 9.14 and 15.61 µm, respectively. The zeta potential of uncoated and coated microparticles was observed to be -26.78 and -29.36 mV, respectively. The prepared coated microparticles decreased the levels of lipid peroxides, MPO, and GSH significantly in colitis. In the Caco-2 cell culture model, the concentration of IL-8 is decreased significantly. The hematological observations confirmed that the prepared formulation showed a promising decrease in the levels of WBC, CRP, and ESR in diseased animals. Animal experiments revealed that cellulose acetate phthalate coated microparticles of mesalamine and S. boulardii significantly improved the colitis disease conditions of Wistar rats. Hence, cellulose acetate phthalate-coated microparticles of mesalamine and S. boulardii could be recommended as adjuvant therapy to achieve a synergistic effect in the management of UC. Lay summary Mesalamine is the drug of choice for the management of ulcerative colitis (UC), which inhibits mediators responsible for inflammation. We investigated the in vivo effects of cellulose acetate phthalate-coated microparticles of mesalamine with Saccharomyces boulardii (probiotic) for their efficacy against UC. Our findings evidenced that the combination of mesalamine with S. boulardii showed a synergistic effect in the 2,4,6- trinitrobenzene sulfonic acid-induced colitis model by reducing the inflammation and maintains the macroscopic features. From the observed results, it can be concluded that S. boulardii can be used to enhance the individual drug's effect in the therapeutic management of UC.

Pharmacological properties of Centella asiatica hydrogel in accelerating wound healing in rabbits.

BACKGROUND: Various extracts of Centella asiatica (Apiaceae) and its active constituent, asiaticoside, have been reported to possess wound healing property when assessed using various in vivo and in vitro models. In an attempt to develop a formulation with accelerated wound healing effect, the present study was performed to examine in vivo efficacy of asiaticoside-rich hydrogel formulation in rabbits. METHODS: Asiaticoside-rich fraction was prepared from C. asiatica aerial part and then incorporated into polyvinyl alcohol/polyethylene glycol (PVA/PEG) hydrogel. The hydrogel was subjected to wound healing investigation using the in vivo incision model. RESULTS: The results obtained demonstrated that: i) the hydrogel formulation did not cause any signs of irritation on the rabbits' skin and; ii) enhanced wound healing 15% faster than the commercial cream and > 40% faster than the untreated wounds. The skin healing process was seen in all wounds marked by formation of a thick epithelial layer, keratin, and moderate formation of granulation tissues, fibroblasts and collagen with no fibrinoid necrosis detected. CONCLUSION: The asiaticoside-rich hydrogel developed using the freeze-thaw method was effective in accelerating wound healing in rabbits.