Study on Novel Nanoparticle Slow-Release Drugs for Moyamoya Disease

Spontaneous basilar artery occlusive disease is a disease characterized by thickening of the intima of the bilateral internal carotid artery and the anterior and middle cerebral arteries, gradually narrowing the arterial diameter, and compensatory dilatation of the perforating artery at the base of the brain. Aspirin (acetylsalicylic acid), as a classic non-steroidal anti-inflammatory drug, has been proven to have antiplatelet, anti-inflammatory, and immune-regulating effects. But how to achieve long-term sustained release of aspirin and achieve anti-platelet aggregation remains to be studied. This study intends to build a microsphere sustained-release system to achieve long-term stable and slow release of aspirin drug, thereby achieving a more ideal anti-platelet aggregation effect. The therapeutic effects of three groups of nanoparticle sustained-release drug regimens on platelet aggregation were compared. The results showed that the platelet inhibition rate and NIHSS scores before treatment were compared between the three groups; compared with the other groups, the PLGA group had higher AA and ADP pathway-induced platelet inhibition rates after treatment and lower plasma Lp-PLA2 and NIHSS scores. This shows that aspirin nanoparticle slow-release drugs can effectively increase platelet inhibition rate and improve the antiplatelet ability of patients with spontaneous basilar artery occlusive disease, which is beneficial to promoting prognosis recovery.

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Evaluating the Mucoprotective Effects of Glycyrrhizic Acid Loaded Polymeric Nanoparticles Against 5-Fluorouracil Induced Intestinal Mucositis in Murine Model via Suppression of Inflammatory Mediators and Oxidative Stress

10.21203/rs.3.rs-262247/v1 ◽

2021 ◽

Author(s):

Mahira Zeeshan ◽

Ayesha Atiq ◽

Qurat Ul Ain ◽

Jawad Ali ◽

Salman Khan ◽

...

Keyword(s):

Drug Delivery ◽

Sustained Release ◽

Inflammatory Mediators ◽

Glycyrrhizic Acid ◽

Plga Nanoparticles ◽

Therapeutic Effects ◽

Therapeutic Action ◽

Polymeric Nanocarriers ◽

Intestinal Mucositis ◽

Anti Inflammatory

Abstract Objectives: 5-Flourouracil (5-FU), a chemotherapeutic drug, is linked with severe deteriorating effects on intestine leading to mucositis. Further, Glycyrrhizic acid is a renown herbal medicine with combined mucoprotective, antioxidant and anti-inflammatory actions, however associated with pharmacokinetics limitations. Owing to its remarkable therapeutic action in inflammatory bowel disease inside the polymeric nanocarriers, we have tried to explore its activity against 5-FU led intestinal mucositis. Polymeric nanocarriers proved to be efficient drug delivery vehicles for long-term remedy against inflammatory diseases, however, yet not explored for 5-FU induced mucositis. Therefore, the study aimed to produce Glycyrrhizic acid loaded poly lactic-co-glycolic acid (GA-PLGA) nanoparticles to evaluate its protective and therapeutic effects on intestinal mucosa against 5-FU mediated mucositis. Methods: For the said purpose, GA-PLGA nanoparticles were prepared using modified double emulsion method, physicochemically characterized and tested for invitro drug release. Thereafter, mucositis was induced by 5-FU (50 mg/kg; IP) administration to the mice for the first three days (day 0, 1, 2) and orally treated with GA-PLGA nanoparticles till seventh day (day 0-6). Results: GA-PLGA nanoparticles significantly reduced mucositis severity as manifested through recovered body weight, diarrhea score, distress, and anorexia. Further, 5-FU induced intestinal histopathological damage, altered villi-crypt length, low goblet cell count, elevated pro-inflammatory mediators and suppressed antioxidant enzymes were reversed by GA-PLGA nanoparticles’ sustained release therapeutic action. Conclusion: Morphological, behavioral, histological, and biochemical results suggested that GA-PLGA nanoparticles found to be efficient, biocompatible, targeted, sustained release drug delivery nano-vehicle for enhanced mucoprotective, anti-inflammatory and antioxidant effects in ameliorating 5-FU intestine mucositis.

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Anti-inflammatory effect of Sustained release granules of Aceclofenac in Gouty Arthritis Rat

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00996 ◽

2021 ◽

pp. 5729-5732

Author(s):

Rajiv Kumar ◽

Parminder Nain ◽

Jaspreet Kaur ◽

Ravi Kumar Dhawan

Keyword(s):

Sustained Release ◽

Therapeutic Effect ◽

Slow Release ◽

Standard Dose ◽

Gouty Arthritis ◽

Control Group ◽

Monosodium Urate ◽

Sustained Release Formulation ◽

Anti Inflammatory ◽

Inflammatory Effect

Gout is most common painful clinical syndrome occurs due to hyperuricaemia (high serum uric acid level) and deposition of monosodium urate crystals in joints. In the current experimental study, the anti-inflammatory effect of sustained release granules of aceclofenac, was investigated on monosodium urate crystal-induced inflammation in rat. Monosodium urate is injected appropriately at a dose of 3 mg/kg body weight of a rat on right ankle to induce inflammation in joint like gouty arthritis. The percentage of joint swelling in positive control group was increased significantly (p<0.5) when compared with normal group after 1 hr, 12 hr and 24 hr with a single injection of MSU. Therapeutic effect of sustained released granules (OD) is similar to conventional released granules (BD) and possesses an anti-inflammatory effect, which could provide relief in gouty arthritis after administration of sustained release formulation of aceclofenac once in a day only. The current study clearly indicated that slow release granules of aceclofenac exerted a strong anti-inflammatory effect against gouty arthritis at standard dose once daily. It concluded that, when aceclofenac tablet is formulated with slow release granules it decreases the dosing frequency with same therapeutic effect.

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Sustained Release Methylphenidate

Child Psychology and Psychiatry Review ◽

10.1017/s1360641700002264 ◽

2000 ◽

Vol 5 (3) ◽

pp. 108-113 ◽

Cited By ~ 2

Author(s):

Tamsin Ford ◽

Eric Taylor ◽

Jody Warner Rogers

Keyword(s):

United Kingdom ◽

Sustained Release ◽

Clinical Guidelines ◽

Slow Release ◽

Therapeutic Effects ◽

The United Kingdom ◽

Multiple Doses

As sustained methylphenidate becomes available in the United Kingdom, there is likely to be considerable demand related to the difficulties that frequently arise with standard methylphenidate due to the need for midday doses at school, as well as the pronounced ‘on/off’ therapeutic effects sometimes seen with multiple doses. This article briefly discusses longer acting stimulants, reviews the available literature, anticipates possible problems in the use of slow release methylphenidate, and presents clinical guidelines for its use.

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Preparation and Evaluation of Physicochemical Properties of the Doxepin Mucoadhesive Gel

Jundishapur Journal of Natural Pharmaceutical Products ◽

10.5812/jjnpp.66864 ◽

2020 ◽

Vol 15 (4) ◽

Author(s):

Majid Rajaee ◽

Amir Talachi ◽

Abbas Pardakhty ◽

Ehsan Mohajeri ◽

Negar Dehghannoudeh ◽

...

Keyword(s):

Physicochemical Properties ◽

Oral Mucosa ◽

Slow Release ◽

Hydroxypropyl Methylcellulose ◽

Poloxamer 407 ◽

Therapeutic Effects ◽

Long Term Effects ◽

Preparation And Evaluation

Background: Oral mucositis is a common debilitating complication of cancer chemotherapy and radiotherapy that can reduce the quality of patient’s lives. Hence, treating this condition plays an important role in increasing the patient’s tolerance. Objectives: Doxepin mucoadhesive gel is useful for treating oral mucosa inflammation caused by long-term effects of chemotherapy, which has low adverse effects. Methods: Doxepin gel’s formulation was prepared with various concentrations of poloxamer 407 and hydroxypropyl methylcellulose in deionized water. The prepared gels were evaluated for pH, appearance, viscosity, spreadability, stability, and drug release. Results: After providing gels containing doxepin, formulations 1, 2, 8, and 9 had low quality and, thus, were removed from the study. Based on qualitative evaluations, formulations 3 and 4 did not meet the criteria for mucoadhesive gel and were removed from the study. The best formulation contained 17% w/w poloxamer 407, 10% w/w hydroxypropyl methylcellulose, and 5% w/w doxepin. Conclusions: Suitable physicochemical properties of prepared doxepin mucoadhesive gel enable it to well cover inflamed and damaged oral mucosa. On the other hand, doxepin’s slow release from formulation (8 hours) can increase therapeutic effects and reduce side effects, which can heal and soothe inflammations of the oral mucosa and be useful in cancer patient’s treatment.

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Analgesic Mechanisms of Steroid Ointment against Oral Ulcerative Mucositis in a Rat Model

International Journal of Molecular Sciences ◽

10.3390/ijms222212600 ◽

2021 ◽

Vol 22 (22) ◽

pp. 12600

Author(s):

Mako Naniwa ◽

Chihiro Nakatomi ◽

Suzuro Hitomi ◽

Kazunari Matsuda ◽

Takuya Tabuchi ◽

...

Keyword(s):

Inflammatory Responses ◽

Therapeutic Effects ◽

Human Volunteers ◽

History Of ◽

Trigeminal Ganglion Neurons ◽

Anti Inflammatory ◽

Hypertonic Stimulation ◽

History Of Use ◽

Ganglion Neurons

Despite the long history of use of steroid ointments for oral mucositis, the analgesic mechanism has not been fully elucidated. In this study, we examined the effects of triamcinolone acetonide (Tmc) on oral ulcerative mucositis-induced pain in conscious rats by our proprietary assay system. Based on evaluations of the physical properties and retention periods in the oral mucosa of human volunteers and rats, we selected TRAFUL® ointment as a long-lasting base. In oral ulcerative mucositis model rats, TRAFUL® with Tmc suppressed cyclooxygenase-dependent inflammatory responses with upregulations of glucocorticoid receptor-induced anti-inflammatory genes and inhibited spontaneous nociceptive behavior. When an ointment with a shorter residual period was used, the effects of Tmc were not elicited or were induced to a lesser extent. Importantly, TRAFUL® with Tmc also improved oral ulcerative mucositis-induced mechanical allodynia, which has been reported to be independent of cyclooxygenase. Ca2+ imaging in dissociated trigeminal ganglion neurons showed that long-term preincubation with Tmc inhibited the hypertonic stimulation-induced Ca2+ response. These results suggest that the representative steroid Tmc suppresses oral ulcerative mucositis-induced pain by general anti-inflammatory actions and inhibits mechanical sensitivity in peripheral nerves. For drug delivery, long-lasting ointments such as TRAFUL® are needed to sufficiently induce the therapeutic effects.

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