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"suppository"
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Achievements in Thermosensitive Gelling Systems for Rectal Administration
by
Bialik, Maria
,
Oledzka, Ewa
,
Sobczak, Marcin
in
Acrylic Resins - chemistry
,
Administration, Rectal
,
Alginates - chemistry
2021
Rectal drug delivery is an effective alternative to oral and parenteral treatments. This route allows for both local and systemic drug therapy. Traditional rectal dosage formulations have historically been used for localised treatments, including laxatives, hemorrhoid therapy and antipyretics. However, this form of drug dosage often feels alien and uncomfortable to a patient, encouraging refusal. The limitations of conventional solid suppositories can be overcome by creating a thermosensitive liquid suppository. Unfortunately, there are currently only a few studies describing their use in therapy. However, recent trends indicate an increase in the development of this modern therapeutic system. This review introduces a novel rectal drug delivery system with the goal of summarising recent developments in thermosensitive liquid suppositories for analgesic, anticancer, antiemetic, antihypertensive, psychiatric, antiallergic, anaesthetic, antimalarial drugs and insulin. The report also presents the impact of various types of components and their concentration on the properties of this rectal dosage form. Further research into such formulations is certainly needed in order to meet the high demand for modern, efficient rectal gelling systems. Continued research and development in this field would undoubtedly further reveal the hidden potential of rectal drug delivery systems.
Journal Article
British Society of Gastroenterology consensus guidelines on the management of inflammatory bowel disease in adults
by
Garrick, Vikki
,
Butterworth, Jeffrey R
,
Brookes, Matthew
in
5-aminosalicylate
,
5-ASA
,
adalimumab
2019
Ulcerative colitis and Crohn’s disease are the principal forms of inflammatory bowel disease. Both represent chronic inflammation of the gastrointestinal tract, which displays heterogeneity in inflammatory and symptomatic burden between patients and within individuals over time. Optimal management relies on understanding and tailoring evidence-based interventions by clinicians in partnership with patients. This guideline for management of inflammatory bowel disease in adults over 16 years of age was developed by Stakeholders representing UK physicians (British Society of Gastroenterology), surgeons (Association of Coloproctology of Great Britain and Ireland), specialist nurses (Royal College of Nursing), paediatricians (British Society of Paediatric Gastroenterology, Hepatology and Nutrition), dietitians (British Dietetic Association), radiologists (British Society of Gastrointestinal and Abdominal Radiology), general practitioners (Primary Care Society for Gastroenterology) and patients (Crohn’s and Colitis UK). A systematic review of 88 247 publications and a Delphi consensus process involving 81 multidisciplinary clinicians and patients was undertaken to develop 168 evidence- and expert opinion-based recommendations for pharmacological, non-pharmacological and surgical interventions, as well as optimal service delivery in the management of both ulcerative colitis and Crohn’s disease. Comprehensive up-to-date guidance is provided regarding indications for, initiation and monitoring of immunosuppressive therapies, nutrition interventions, pre-, peri- and postoperative management, as well as structure and function of the multidisciplinary team and integration between primary and secondary care. Twenty research priorities to inform future clinical management are presented, alongside objective measurement of priority importance, determined by 2379 electronic survey responses from individuals living with ulcerative colitis and Crohn’s disease, including patients, their families and friends.
Journal Article
A prospective study of vaginal topical pretreatment of compound sea-buckthorn oil suppository in postmenopausal women prior to colposcopy
2025
Postmenopausal women are faced with difficulties in colposcopy, such as easy bleeding from epithelial atrophy, and thinning, atypical colposcopy images, unsatisfactory exposure, and decreased sensitivity of colposcopy. We aimed to improve the sensitivity and satisfaction of colposcopy in postmenopausal women and to evaluate the clinical efficacy of compound sea-buckthorn oil suppository on topical vaginal pretreatment in postmenopausal women prior to colposcopy. Postmenopausal patients who underwent colposcopy in the Obstetrics and Gynecology Hospital of Fudan University from April 2023 to July 2024 were randomly assigned to three groups: (A) untreated control group, (B) compound sea-buckthorn oil suppository group, (C) estrogen ointment group. Group B and group C were treated for 2 weeks before colposcopy, and the colposcopy and adverse reactions were analyzed. A total of 377 patients were included in this study, of which 9 patients were excluded from the colposcopy results for failing to complete the 2-week medication, and 368 patients were included in the colposcopy results, including 125 patients in group A, 121 patients in group B, and 122 patients in group C. The high-risk HPV infection before colposcopy accounted for 94.3% (347/368), of which HPV16 and/or HPV18 infection accounted for 20.4% (75/368), and other types of infection accounted for 75.3% (277/368). The patients with abnormal cytology (ASCUS and above) accounted for 47.6% (175/368). No significant differences were observed in age, cytology before colposcopy, and HPV type among the three groups. There were 196 cases (53.3%) of abnormal pathologies in postoperative colposcopic biopsy, among which 42 cases were high-grade cervical squamous intraepithelial lesions. After 2 weeks of medication, the integrity of vaginal epithelium, the adequacy ratio of colposcopy, and the satisfaction rate of acetic acid test and iodine staining test in groups B and C were significantly improved compared with group A (
P
< 0.001), and there was no significant difference between groups B and C. The incidence of breast discomfort in the estrogen ointment group was 5.6%, while the incidence of dizziness and headache was 4%. In contrast, no such side effects were reported in the compound sea-buckthorn oil suppository group, and the difference was statistically significant. Additionally, there was no significant statistical difference in local vaginal adverse reactions between groups B and C. Compound sea-buckthorn oil suppositories are helpful in improving the sensitivity and satisfaction of postmenopausal women with colposcopy, reduce blind biopsies. The effects are not inferior to estrogen. Compared to estrogen ointment, compound sea-buckthorn oil suppositories are most cost-effective and have fewer side effects and can be applied in clinical practice.
Journal Article
VagiBIOM Lactobacillus suppository improves vaginal health index in perimenopausal women with bacterial vaginosis: a randomized control trial
2024
Bacterial vaginosis (BV) can cause vaginal dysbiosis that may influence general vaginal health and pregnancy complications. Balancing vaginal microbiome using
Lactobacillus
spp. may be a new way to prevent and treat mild BV. We conducted a randomized, double-blind, placebo-controlled pilot study aimed at evaluating the effect of the product VagiBIOM, a multi-
Lactobacillus
vaginal suppository, on peri- and premenopausal women with BV in restoring vaginal pH and overall vaginal health by resetting the vaginal microbiome composition. Sixty-six peri- and premenopausal women with BV symptoms were randomized with a 2:1 ratio to be treated with VagiBIOM or placebo suppositories. Vaginal pH, VAS itching score, total Nugent score, and vaginal health index (VHI) were measured. Vaginal microbiome changes before and after the treatment were analyzed by 16S rRNA sequencing and bioinformatics analysis. After 4 weeks of intervention with VagiBIOM or a placebo, the mean score for vaginal pH, VAS itching, and total Nugent score was significantly decreased from the baseline. Compared to the baseline scores, the VHI scores improved significantly following 28-day intervention (
p
< 0.001). Our results revealed two
Lactobacillus
species,
L. hamsteri,
and
L. helveticus
, as indicator species occurring differentially in the VagiBIOM-treated group. Furthermore, the regression and species network analyses revealed significant bacterial associations after VagiBIOM treatment.
Lactobacillus hamsteri
was positively associated with the Nugent score and negatively associated with vaginal pH.
L. iners
and
L. salivarius
were positively and inversely associated with VHI. As is typical,
Bacteroides fragilis
was positively associated with vaginal pH and negatively associated with the Nugent score. Interestingly, the
Lactobacillus
spp. diversity improved after VagiBIOM treatment. The VagiBIOM suppository treatment for peri- and premenopausal women with BV significantly relieved vaginal itching by decreasing vaginal pH and Nugent scores and improving the overall VHI after 4 weeks’ intervention. This effect was primarily the result of VagiBIOM improving vaginal
Lactobacillus
diversity.
Trial Registration
ClinicalTrials.gov registration: NCT05060029, first registration 09/28/2021: Title: A Pilot Study to Evaluate the Efficacy and Safety of Lactobacillus Species Suppositories on Vaginal Health and pH.
Journal Article
Rectal delivered nanocomposite suppository against radiation-induced proctitis
2026
Background
Radiation-induced proctitis is a common complication of radiotherapy for pelvic malignancies, for which effective local treatments remain limited. Epigallocatechin gallate (EGCG) has antioxidant and anti-inflammatory activities but is limited by poor stability and bioavailability. This study aimed to develop a stable, rectally deliverable EGCG-based formulation to mitigate radiation-induced rectal injury.
Results
An EGCG–zinc (EGCG–Zn) nanocomplex was prepared via metal–polyphenol coordination and formulated into a thermosensitive rectal suppository for localized delivery. Zinc coordination significantly improved EGCG stability while preserving its antioxidant activity. The suppository enabled prolonged rectal residence and enhanced local drug exposure. In irradiated mouse models, EGCG–Zn suppositories reduced oxidative stress, DNA damage, and inflammatory responses in rectal tissue, and promoted epithelial regeneration and tight junction restoration. Transcriptomic and molecular analyses suggested involvement of inflammation-related and epithelial barrier–associated signaling pathways. No detectable local or systemic toxicity was observed after repeated administration.
Conclusions
These findings indicate that an EGCG–Zn–based thermosensitive rectal suppository is a safe and effective localized strategy for alleviating radiation-induced proctitis, with potential translational value for the management of radiation-associated rectal injury.
Graphical Abstract
Schematic illustration of a temperature-sensitive EGCG–Zn nanocomposite suppository for rectal administration and its protective effects against radiation-induced proctitis by scavenging reactive oxygen species, inhibiting inflammation, and promoting intestinal barrier repair
Journal Article
Pathways for Oral and Rectal Delivery of Gold Nanoparticles (1.7 nm) and Gold Nanoclusters into the Colon: Enteric-Coated Capsules and Suppositories
by
Heggen, Marc
,
Kostka, Kathrin
,
Wetzel, Oliver
in
Administration, Oral
,
capsules
,
Capsules - chemistry
2021
Two ways to deliver ultrasmall gold nanoparticles and gold-bovine serum albumin (BSA) nanoclusters to the colon were developed. First, oral administration is possible by incorporation into gelatin capsules that were coated with an enteric polymer. These permit the transfer across the stomach whose acidic environment damages many drugs. The enteric coating dissolves due to the neutral pH of the colon and releases the capsule’s cargo. Second, rectal administration is possible by incorporation into hard-fat suppositories that melt in the colon and then release the nanocarriers. The feasibility of the two concepts was demonstrated by in-vitro release studies and cell culture studies that showed the easy redispersibility after dissolution of the respective transport system. This clears a pathway for therapeutic applications of drug-loaded nanoparticles to address colon diseases, such as chronic inflammation and cancer.
Journal Article
Investigation into the pharmacodynamics and pharmacokinetics of recombinant human interferon alfa-2b vaginal suppository following process optimization in chinese rhesus macaque
2025
Recombinant human interferon Alfa-2b vaginal suppository is a gynecological preparation mainly made of interferon, commonly used to treat diseases related to viral infections such as cervical erosion. As a recombinant protein drug, it is important to pay attention to the possibility of modifications that may lower the quality of the drug during the production process. The aim of this study is to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of this product in Chinese rhesus macaque after purification process changes, and to demonstrate that there is no difference in the biological activity of recombinant human interferon Alfa-2b vaginal suppository stock solution before and after process changes. There are 12 test animals: Chinese rhesus macaques who received a two-group crossover design and were subcutaneously injected with the same active dose of 500,000 IU/kg around the navel in the abdomen. According to maximum concentration (C
max
) and time of maximum concentration (T
max
) within non-parametric test (
P
> 0.05), geometric mean ratio of PK parameter C
max
for the drugs after purification process changes (sample S) compared to the before purification process changes one (sample R) was 97.09%, with a 90% confidence interval (CI) of 87.39–107.87%. The geometric mean ratio C
max
of serum Beta2-microglobulin (PD
max
) for PD index is 100.07%, with a 90% CI of 97.16–103.07%; Geometric mean ratio of AUEC
0 − t
is 98.91%, with a 90% CI of 96.53–101.34%. The geometric mean of the PD index, neopterin PD
max
, is 97.75%, with a 90% CI of 92.53–103.25%; Geometric mean of AUEC
0 − t
is 105.59%, with a 90% CI ranging from 97.22 to 114.68%. The important parameters of PK/PD meet the equivalence requirements, and biological activity of the recombinant human interferon Alfa-2b vaginal suppository stock solution after purification process change is no different from before the change. Under the same active dose administration conditions, the same biological effects were produced, achieving the same effect as before the change.
Journal Article
Development and Comprehensive Characteristics of Thermosensitive Liquid Suppositories of Metoprolol Based on Poly(lactide-co-glycolide) Nanoparticles
2022
Thermosensitive liquid suppositories (LSs) carrying the model antihypertensive drug metoprolol tartrate (MT) were developed and evaluated. The fundamental purpose of this work was to produce, for the first time, liquid MT suppositories based on biodegradable nanoparticles and optimize their rheological and mechanical properties for prospective rectal administration. The nanoparticle system was based on a biodegradable copolymer synthesized by ring opening polymerization (ROP) of glycolide (GL) and L,L-lactide (LLA). Biodegradable nanoparticles loaded with the model drug were produced by the o/o method at the first stage of the investigation. Depending on the concentration of the drug in the sample, from 66 to 91% of MT was released over 12 h, according to first-order kinetics. Then, thermosensitive LSs with MT-loaded biodegradable nanoparticles were obtained by a cold method and their mechanical and rheological properties were evaluated. To adjust the thermogelling and mucoadhesive properties for rectal administration, the amounts of major formulation components such as poloxamers (P407, P188), Tween 80, hydroxypropylcellulose (HPC), polyvinylpyrrolidone (PVP), and sodium alginate were optimized. The in vitro release results revealed that more than 80% of the MT was released after 12 h, following also first-order kinetics. It was discovered that the diffusion process was dominant. The drug release profile was mainly governed by the rheological and mechanical properties of the developed formulation. Such a novel, thermosensitive formulation might be an effective alternative to hypertension treatment, particularly for unconscious patients, patients with mental illnesses, geriatric patients, and children.
Journal Article
Preparations of Rectal Suppositories Containing Artesunate
2020
Rectal artesunate suppositories are a useful option for pre-referral treatment of severe malaria, specifically in children under 6 years of age in remote malaria-endemic areas. The main challenges are to improve the solubility of drugs in the rectal fluids and prevent the product from turning rancid or melting in a tropical climate. In this short proof-of-concept study, three types of rectal suppositories of artesunate were prepared: (i) polyethylene glycol (PEG)-based suppositories carrying free artesunate (non-modified artesunate), (ii) PEG-based suppositories carrying artesunate-loaded micelles and (iii) 3D-printed suppositories carrying a PEG/artesunate mixture. Physical parameters of suppositories, release profiles of artesunate (the fastest to the slowest: ii≥i>iii) and thermostability (the most stable to the least stable: iii>ii>i) of suppositories at increased temperature were assessed to determine the advantages and disadvantages of each formulation.
Journal Article