Solidified reverse micellar solutions (SRMS): A novel approach for controlling drug release from various lipids based drug delivery systems

Solidified reverse micellar solutions (SRMS) are reverse micelles containing lecithin and a triglyceride, for example, SOFTISAN®142, which is hydrogenated coco glyceride. SRMS transform into a lamellar mesophase after melting on contact with water; this transformation enables controlled release of solubilized drugs. They offer potentials for sustained drug delivery of both hydrophilic and lipophilic drugs. SRMS have the advantage of providing more flexibility in controlling the drug release and protecting the encapsulated ingredients from chemical degradation. SRMS based systems influence the absorption of active ingredients through different mechanisms to modify the release of active ingredients, and improve drugs bioavailability. The types of SRMS-based drug delivery systems include solid lipid nanoparticles (SLN), solid lipid microparticles (SLM), tablets and suppositories amongst others. The work exhaustively reviews the advances in SRMS based carriers. Its formulation methods, characterisation and delivery systems were discussed in details.Key words: Solidified reverse micellar solutions (SRMS), lipids, wide angle X-ray diffraction analysis (WAXD), small angle X-ray diffraction analysis (SAXD), lipid absorption

IN VITRO PROPERTIES OF SOLID LIPID MICROPARTICLES (SLMS) LOADED WITH METHANOLIC EXTRACT OF GARCINIA KOLA (HECKEL) SEED

Objective: The decline in the use of herbal medicine especially in the Western world may be due to lack of readily available market brand formulations and the fact that most herbal remedies are taken as tea, decoctions and infusions. The taste of some of these herbal drugs is not palatable, and some have unpleasant odour and colour hence, the need to formulate these drugs in form of encapsulated dosage forms. The objective of the work was to formulate solid lipid microparticles (SLMs) loaded with the methanolic extract of Garcinia kola seed. Methods: The SLMs containing 1 and 3 % of Garcinia kola seed extract were formulated using fat from Capra hircus and Phospholipon® 90H (3:1). The particle morphology and size, encapsulation efficiency (EE%), pH, in vitro release and the inhibition zone diameter (IZD) of the SLMs were determined. Results: The results showed that the extract was very bitter while, the encapsulated G. kola had slight bitter taste. The pH remained in the acidic region from 1 to 30 days. Particle size of 28.65 ± 1.13 and 29.49 ± 1.24 µm were obtained for SLMs loaded with 1 and 3 % of the extract respectively. SLMs had high EE% of 94 % and also exhibited good release of the extract in simulated intestinal fluid (SIF, pH 7.2). Garcinia kola-loaded SLMs had good activity against Staphylococcus aureus and no action against Escherichia coli. Conclusion: Therefore, Garcinia kola seed extract could be formulated as SLMs in order to mask its bitter taste and improve compliance. Â

SUSTAINED RELEASE ARTEMETHER-LOADED SOLID LIPID MICROPARTICLES, BASED ON SOLIDIFIED REVERSE MICELLAR SOLUTION (SRMS)

Objectives: To prepare and evaluate sustained release artemether-loaded SLMs based on SRMS Material and methods: SRMS, consisting of mixtures of Phospholipon® 90H (P90H) and Softisan® 154 (1:1, 2:1 and 1:2) were formulated and characterized using differential scanning calorimetry (DSC). The SRMS were used to formulate artemether-loaded SLMs by melt homogenization. The SLMs were characterized based on particle size and morphology, pH stability, encapsulation efficiency (EE%) and loading capacity. In vitro release was carried out in simulated intestinal fluid (SIF, pH 7.5). Results: Thermograms of the SRMS (1:1, 2:1 and 1:2) showed sharp endothermic peaks at 65.5, 64.4 and 62.3 oC respectively. Maximum EE% of 70.00 ± 1.50 % was obtained for SLMs formulated with SRMS 1:1 and 1 % artemether. Loading capacity ranged from 5.67 to 17.90 g drug/100 g lipid. In vitro release showed about 80 to 84 % drug release at 7 h. Particle size of artemether-loaded SLMs ranged from 18.60 ± 0.09 to 34.80 ± 0.30 µm. The pH decreased significantly at 60 days from 6 to 4.8 for batch A2 formulated with SRMS 2:1 and 3 % artemether (p < 0.05). Conclusion: artemether-loaded SLMs based on SRMS had good sustained release properties and could be used once daily in order to enhance patient's compliance.   Key words: Malaria, artemether, SRMS, lipids, sustained release SLMs Â

Recent advances in particulate anti-malarial drug delivery systems: A review

Malaria remains a tremendous health burden in tropical areas, causing a life-threatening disease and accounts for 1 to 2 million deaths round the globe yearly. Researchers have explored different novel approaches to deliver and improve the biopharmaceutical performance of drugs used in malaria chemotherapy. These novel drug delivery systems (NDDS) enhanced bioavailability of these drugs and also may offer controlled release of these drugs. The major aim of the NDDS is to improve the efficacy of these drugs, and at the same time to eliminate their toxicity. These NDDS include: micro/nanoparticulate DDS, emulsion based DDS, dendrimers and liposomes among others. The development of these particulate carriers as vehicles for the delivery of active compounds is a novel area of research that provides a new hope in malarial chemotherapy. The work presents various trends in malarial chemotherapy, as well as an exhaustive screening of different particulate drug delivery systems (PDDS) and the recent advances in the delivery of anti-malarial drugs using the novel particulate drug delivery systems (NPDDS)

Preliminary spectroscopic characterization of PEGylated mucin, a novel polymeric drug delivery system

The objective of this study was to evaluate, spectrophotometrically, the compatibility of non-mucinated polyethylene glycol (PEG) 4000 and non-PEGylated mucin in a PEGylated mucin matrices for drug delivery application. Mucin was extracted from the giant African land snails (Archachatina maginata) using chilled acetone and characterized in terms of qualitative properties and solubility profile. Polymeric matrices composed of PEG 4000 and mucin in ratios of 2:0 (A), 1:1 (B), 2:1(C) and 3:1 (D) were prepared by co-precipitation using chilled acetone. The matrices were characterized with respect to compatibility using the Fourier transform infrared (FT-IR) spectroscopy. Results of the qualitative tests performed on the snail mucin showed that carbohydrates, proteins and trace amounts of fats were present; the extracted mucin was light-brownish in colour, with a pleasant meaty odour. Snail mucin, when dispersed in water yielded a slightly viscous dispersion, but is not soluble in ethanol, acetone, 0.1 M sodium hydroxide, ammonium hydroxide and sulphuric acid. The presence of different peaks in the FT-IR spectra of the PEGylated mucin matrices compared with the non-PEGylated mucin (2:0) matrix and non-mucinated PEG 4000 (0:2) matrix indicated the formation of new polymers, which could be employed in drug delivery. This study has shown that PEGylation of mucin gives rise to new polymeric system with principal FT-IR peaks quite different from those of non-PEGylated mucin and nonmucinated PEG, and this may be employed in the delivery of drugs.Key words: PEGylation, drug delivery, mucin, Fourier transform infrared (FT-IR) spectroscopy, Archachatina maginata

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ABSTRACT The use of traditional medicines and phytopharmaceuticals for treating various ailments dates back several centuries. The aim of the present review is based on relevant data on the different approaches to formulation of various natural compounds from ethnomedicinal plants. Attempts are also being made to enumerate the possible leads from traditional medicinal system for the treatment of diseases. We tried to provide the readers with the array of processes, which can be further worked upon in clinical studies. Finally, this paper puts forth issues that need to be addressed by researchers in the future with respect to standardization of phytopharmaceuticals

EVALUATION OF METRONIDAZOLE TABLETS FORMULATED WITH DIFFERENT DISINTEGRANTS USING MOISTURE ACTIVATED DRY GRANULATION

Introduction:  Metronidazole is a synthetic oral nitroimidazole antibiotic used in the treatment of infections caused by anaerobic bacteria and protozoa. It also has amebicidal and antiprotozoal properties. Aim: The purpose of the study was to formulate and evaluate metronidazole tablets formulated with polymers (PVP and PEG) and maize starch as disintegrant using moisture activated dry granulation (MADG). Method: Twenty-four (24) batches of metronidazole granules and tablets were prepared by moisture activated dry granulation.  Metronidazole (200 mg), lactose and gelatin (1, 2, 4, and 8 %) were mixed, followed by continuous mixing. Prior to compression, micro-crystalline cellulose, disintegrants and magnesium stearate were added. The dried granules were passed via 1.0 mm sieve after which they were labelled and stored in an air tight container. All other batches were also similarly prepared. Result: The result showed that the mean weight of the tablets ranged from 0.33±0.01 to 0.35±0.04 g. Tablet hardness ranged from 5.00±0.85 to 6.36±1.43. The results showed that batch 11 tablets had higher crushing strength than batch 24 with a significant difference. Table 2 shows the hardness test results and clearly indicates that the results of all the samples significantly differ from each other (p<0.05). The tablet friability test ranged from 0.21±0.17 for batch 24 and 0.60±0.16 for batch 11.  The formulated tablets showed average disintegration time ranges from 0.52±0.01 to 14.03±0.03. According to USP, the disintegration time must be in the range of 15 min for uncoated tablets, and 30 mins for film coated tablets. Conclusion: The study established that polyethylene glycol and polyvinyl pyrrolidone polymers had better dissolution profile than maize starch which has the best disintegration properties.                          Peer Review History: Received: 4 March 2023; Revised: 26 April; Accepted: 20 June 2023, Available online: 15 July 2023 Academic Editor: Dr. Jennifer Audu-Peter, University of Jos, Nigeria, [email protected] Received file:                             Reviewer's Comments: Average Peer review marks at initial stage: 5.0/10 Average Peer review marks at publication stage: 7.0/10 Reviewers: Dr. Julie Ann S. Ng, Blk 18 Lot 6 Grandville 3 Subdivision Mansilingan, Bacolod City, Philippines.  [email protected] Dr. Essam Mohamed Eissa, Beni-Suef – 32 Tahrir St, Egypt, [email protected]