Bone, skin and soft tissue chronic wounds emanating from burns or bacterial infections which persist due to prolonged tissue inflammation contribute to a delay in wound healing. Electrospun biomimetic scaffolds produced from biodegradable polymers have proven to be a better alternative due to their large surface area to volume ratio and ability to release the drug directly to the wound surface allowing fast and sustained absorbance over the affected wound area. In this study, poly lactic acid (PLA) (20% w/v) and collagen-based (PLA/C) fibrous scaffolds (electrospun at a voltage of 22 kV, flow rate of 0.1 mL/min) containing varying concentrations of silver sulphadiazine (1% w/w, 0.75% w/w) (Ag + S) and Aspalathus linearis (AL) fermented extract (0.025%, 0.1% and 0.5% w/w), were designed and fabricated to increase antimicrobial penetration and cellular biocompatibility. The elastic modulus of samples revealed that incorporating 1% Ag + S and A. linearis extract to PLA solution culminates in a fiber with the superlative stiffness of 2.1.1 GPa. The antimicrobial effect of the scaffolds was evaluated against S. aureus, P. aeruginosa, MRSA and E. coli. PLA/C-Ag + S/AL scaffolds and showed antibacterial activity against both gram +ve and gram −ve bacteria. They were nontoxic to the cells and provided favorable substrates for the neonatal epidermal keratinocytes cells to undergo cell attachment and proliferation. PLA/C-Ag + S/AL scaffolds have a great potential for use in chronic wounds as well as in tissue and bioengineering applications.
Background Sexual transmission of HIV is the most common means of acquiring the disease. Topical microbicides have been investigated to prevent transmission. This study will use a specific entry inhibitor, maraviroc, and a nucleotide reverse transcriptase inhibitor (NRTI), tenofovir, a dual combination which will provide a synergist effect that can enhance the efficacy of HIV microbicides via a mucoadhesive dual compartment bigel. Bigel formulation via hydrogel organogel linkages were developed and evaluated for their physicochemical characteristics, safety, and anti-HIV efficacy. In vitro diffusion studies were performed with Franz diffusion cells having effective diffusion surface area of 1.76cm2 and receiver chamber volume of 15mL. Result The bigel formulations showed a viscosity ranging from 14179 to 14560 cPs and had a good spreadability and acidic pH in the range of 4.0 ± 0.34 to 5.2 ± 0.18. The bigel formulations showed good anti-HIV activity at a concentration of 0.1 μg/mL. The in vitro release study of maraviroc from the bigel formulations showed a release rate ranging from 2.675 to 3.838 μg/cm2/min½ while the release rate for tenofovir ranged from 3.475 to 3.825 μg/cm2/min½. The bigel formulations were non-toxic to the human vagina as there was < 1 log10 change in Lactobacilli crispatus viability. Conclusion This study successfully developed a dual compartment bigel containing maraviroc and tenofovir. BG C was found to be stable and safe towards vaginal and rectal epithelium, and it actively prevented HIV transmission. This bigel has the potential for long-term pre-exposure prophylaxis prevention of HIV transmission.
Background: Suitable α-cellulose and microcrystalline cellulose powders for use in the pharmaceutical industry can be derived from agricultural wastes. Aims: The pharmacopoeial and physicochemical properties of cornstalk α-cellulose (CCC) and cornstalk microcrystalline cellulose powders (MCCC) were compared to a commercial brand of microcrystalline cellulose (Avicel PH101) to evaluate their usefulness as pharmaceutical excipients. Settings and Design: Physicochemical properties of an excipient play a very crucial role in the functions of the excipient; hence, these properties were evaluated and compared with a commercial brand. Materials and Methods: α-cellulose was extracted from cornstalks. Modification of this α-cellulose powder was carried out by its partial hydrolysis with hydrochloric acid (HCl) to obtain a microcrystalline cellulose powder. Their pharmacopoeial, physicochemical and microbiological properties were evaluated using standard methods. Statistical Analysis: OriginPro 8 SR2 v. 0891 (B891) software (OriginLab Corporation USA) was used for statistical evaluation. One-way analysis of variance was used to differentiate between samples and decide where significant differences were established. Results: The yield of α-cellulose from the cornstalks was 32.5%w/w and that of microcrystalline cellulose 26%w/w. All the cellulose samples met all the pharmacopoeial parameters that were carried out. The comparison of physicochemical properties of the CCC, MCCC and Avicel PH101 suggests that the microcrystalline celluloses might have better flow and compression properties than the CCC sample. The three cellulose powders were of high microbial excipient quality. For almost all parameters evaluated, it was generally observed that the MCCC has similar characteristics to Avicel PH101. Conclusions: MCCC can be a suitable alternative to the expensive Avicel PH101as pharmaceutical excipients.
Background: In this study, the chronic wound healing ability of PLA-based electrospun nanofibers loaded with hyaluronic acid, valsartan, and ascorbic acid is explored. PLA-based scaffolds were fabricated by electrospinning, followed by loading the scaffolds with different concentrations of hyaluronic acid, valsartan, and ascorbic acid hydrogels. The produced formulations were characterized by scanning electron microscopy imaging (SEM), tensile strength testing, Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). An in vitro drug release study was conducted to monitor the release of valsartan from the different formulations. This was followed by exploring the wound healing effects of the scaffolds in alloxan-induced diabetic rats and comparing the wound healing effects with positive and negative controls. Results: The average diameter of the fibers was in the range of 300 to 490 nm with high porosity in the range of 63.90 to 79.44%, offering a large surface area-to-volume ratio, enhanced drug solubility, oxygen permeability, and fluid uptake. The presence of valsartan significantly impacted on the re-epithelization rate. Percentage reepithelization rate was 31.2% ± 1.77% in the absence of treatment. Histologic section of tissue showed skin with underlying loose fibro-collagenous stroma (dermis) containing sebaceous glands and hair follicles for animals treated with VA, VB, VC, and VD. All the scaffolds reduced the number of inflammatory cell infiltrates at the wound site compared to the no treatment and conventionally treated groups. Conventional antibiotic treatment and VD (electrospun biomimetic scaffolds containing ascorbic acid) had % re-epithelization rates of 59.45% ± 1.69% and 62.01% ± 1.68% which were significantly lower than the PLA/HA-valsartan hydrogel scaffolds with VB having the highest % re-epithelization rate of 85.5% ± 1.7% (Figure 4B & 5C). Conclusion: This study explored the use of biomimetic polylactic acid-based electrospun fiber and HA-valsartan hydrogel scaffold incorporating topical angiotensin receptor blockers to successfully accelerate wound healing. The novel PLA-based electrospun fibers loaded with hyaluronic acid-valsartan hydrogels were stable and possessed proven diabetic wound healing property. This was as a result of the known biomimetic effect of the fibers and increased re-epithelization facilitated by the hydrogels containing valsartan.
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